Jump to content
Main menu
Main menu
move to sidebar
hide
Navigation
Main Page
My Profile
My Assessments
My Life Story
Administer Assessments
Med Classes
Problems
Recent changes
Feature requests
Pharmacopedia
Search
Search
Appearance
Create account
Log in
Personal tools
Create account
Log in
Drilldown: Medicines
English
Tools
Tools
move to sidebar
hide
Actions
General
Printable version
Appearance
move to sidebar
hide
Pharmacopedia
Browse
Categories
Log in
Nav
Pharmacopedia
×
Main
Main page
Medicines A–Z
Categories
Recent changes
My account
Log in
Help
About
Special pages
Feature requests
Choose a table:
Medicines (732)
Medicines
> mechanism:
None
&
onset:
Symptom relief within 30 minutes
&
bioavailability:
High (oral)'"`UNIQ--ref-00000FB5-QINU`"'
Use the filters below to narrow your results.
generic:
Phenazopyridine (1)
brand:
Pyridium (Rx), Azo Standard, AZO Urinary Pain Relief (OTC) (1)
classes:
[[:Category:Azo_dyes|Azo dye]] (1)
·
[[:Category:Urinary_analgesics|Urinary tract analgesic]] (1)
mechanism:
(Click arrow to add another value)
None
·
5-HT2A agonist
·
GABAA positive allosteric modulator
·
Monoamine releasing agent
·
CB1/CB2 agonist
·
Potent mu-opioid receptor agonist
·
Sodium channel blocker
·
Dopamine/norepinephrine reuptake inhibitor
·
GABAA potentiator; NMDA antagonist
·
Phenothiazine D2 antagonist
·
Potent 5-HT2A agonist
·
5-HT1B/1D agonist
·
LSD analogue; 5-HT2A agonist
·
Mu-opioid receptor agonist
·
Muscarinic receptor antagonist
·
Prodrug of LSD; 5-HT2A agonist
·
Selective norepinephrine reuptake inhibitor
·
GABAA positive allosteric modulator (non-benzodiazepine)
·
GABAA potentiator and direct activator
·
Irreversible non-selective MAO inhibitor
Other values:
1-acetyl-LSD; prodrug of LSD
5-HT1A agonist, 5-HT2A antagonist, with weaker activity at D4 and other receptors. Net effect involves enhanced prefrontal dopaminergic/noradrenergic tone with decreased serotonergic inhibition of sexual desire.
5-HT1B/1D agonist; alpha-adrenergic agonist
5-HT1B/1D agonist; long half-life
5-HT1F receptor agonist
5-HT2A agonist; 5-HT3 antagonist
5-HT2A agonist; D2 partial agonist
5-HT2A agonist; MAO inhibitor
5-HT2A agonist; long duration
5-HT2A agonist; milder than other 2C-x
5-HT2A agonist; minor psilocybin mushroom alkaloid
5-HT2A agonist; primarily auditory effects
5-HT2A agonist; sigma-1 agonist
5-HT2A partial agonist
5-HT2A partial agonist; sigma-1 agonist
5-HT2C agonist; 5-HT2A antagonist; serotonin releasing agent
5-MeO-DMT is a potent 5-HT1A agonist (greater than 5-HT2A). Distinct from N,N-DMT in producing a more unitive, less visual, often ego-dissolving experience.
5HT1a
ACTH analogue; BDNF upregulator
AMPA modulator; catecholaminergic
AMPA receptor antagonist
AMPA receptor modulator
AMPA receptor positive allosteric modulator
AMPA/NMDA modulator; NGF/BDNF upregulation
Acetylcholinesterase and butyrylcholinesterase inhibitor
Acetylcholinesterase inhibitor; nicotinic ACh receptor modulator
Active alkaloid is cytisine, a nicotinic acetylcholine receptor agonist. NOT a classical 5-HT2A psychedelic.
Active metabolite of DXM; NMDA antagonist
Active metabolite of tramadol; mu-opioid agonist
Active oils are myristicin, elemicin, and safrole, phenethylamine precursors that may be aminated in vivo to MMDA, TMA, and MDA respectively (Shulgin's 'essential amphetamines' hypothesis).
Active principle is thujone, a GABA-A antagonist (the opposite of most CNS depressants). Also present in cooking sage (''Salvia officinalis''), tansy, and ''Thuja'' cedars.
Adenosine receptor antagonist
Adenosine receptor antagonist; dopaminergic
Adenosine receptor antagonist; phosphodiesterase inhibitor
Agonist at the metabotropic GABAB receptor and the endogenous γ-hydroxybutyrate (GHB) receptor. Produces deep sleep with increased slow-wave architecture, suppression of REM intrusion, and cataplexy reduction.
Agonist of the [[GLP-1 receptor]]; exendin-4 derivative from Gila monster venom.
Aldehyde dehydrogenase inhibitor
Alpha-2 adrenergic receptor agonist
Alpha-adrenergic agonist; monoamine releaser
Alpha-methylated amphetamine analogue; norepinephrine releasing agent
Anticholinergic; NMDA antagonist
Apomorphine and nuciferine; dopaminergic activity
Biphasic activity at CB1: neutral antagonist at low doses, partial agonist at high doses; partial agonist at CB2.
Buprenorphine: high-affinity partial agonist at the μ-opioid receptor with ceiling effect on respiratory depression. Naloxone: abuse-deterrent, inactive SL but precipitates withdrawal if injected.
Butyrophenone D2 antagonist
CB1 partial agonist
CB1 partial agonist (lower potency than delta-9)
CB1/CB2 agonist (higher potency than THC)
CB1/CB2 partial agonist
CGRP receptor antagonist
CNS mechanism incompletely understood
Caffeine (1.5–2%) + theobromine + kolanin (a glycoside).
Caffeine (highest of the ''Ilex'' genus) plus saponins that produce ritual vomiting at high doses.
Caffeine (sometimes called 'mateine' historically, though chemically identical), theobromine, theophylline, plus polyphenols.
Caffeine + theophylline + L-theanine. L-theanine (an amino acid unique to tea) modulates glutamate and produces an 'alpha-wave' calming overlay on caffeine's stimulation, hence tea's reputation as a 'cleaner' stimulant than coffee.
Caffeine is a non-selective adenosine A1/A2A receptor antagonist; also weak PDE inhibition. Beans contain theobromine (3,7-DMX) and theophylline (1,3-DMX) in smaller amounts.
Cardioselective β1-adrenergic antagonist. Selectivity is dose-dependent and partially lost at higher doses.
Cathinone analogue; monoamine reuptake inhibitor
Central and peripheral COMT inhibitor
Cleaves SNAP-25 protein in presynaptic motor and autonomic nerve terminals, blocking acetylcholine release; in chronic migraine, hypothesized to inhibit peripheral sensitization of trigeminovascular nociceptors
Competitive antagonist at OX1R and OX2R. Faster receptor association/dissociation kinetics than suvorexant (~16 sec dissociation vs ~57 sec) hypothesized to support sleep onset, with sufficient duration for maintenance.
Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant.
Competitive mu/kappa/delta opioid receptor antagonist
Contains LSA
Contains atropine, scopolamine, hyoscyamine
Contains bufotenin and DMT
Contains harmine, harmaline, tetrahydroharmine
Contains ibogaine; kappa-opioid agonist
Contains mescaline
Contains muscimol and ibotenic acid
Contains psilocybin and psilocin
Contains salvinorin A
Contains the β-carboline alkaloids harmine, harmaline, and tetrahydroharmine, reversible monoamine oxidase inhibitors (RIMAs) that allow oral DMT to reach the brain.
Contains varying amounts of DMT, 5-MeO-DMT, bufotenine, and gramine depending on strain and growing conditions.
D1/D2/D3 receptor agonist
D2 agonist; D1 partial agonist
D2 receptor agonist
D2 receptor antagonist; also H1, alpha-1, muscarinic antagonist
D2/5-HT2A antagonist
D2/5-HT2A antagonist; 5-HT7 antagonist
D2/5-HT2A antagonist; SRI and NRI
D2/5-HT2A antagonist; active metabolite of risperidone
DMT + MAOI (harmine/harmaline); 5-HT2A agonist
DMT-containing plant used in psychedelic preparations
Dibenzoxazepine D2/5-HT2 antagonist
Dihydroindolone D2 antagonist
Diphenhydramine salt; H1 antagonist
Diphenylbutylpiperidine D2 antagonist
Donepezil: reversible AChE inhibitor, increases synaptic acetylcholine. Memantine: uncompetitive low-affinity NMDA receptor antagonist, dampens pathological glutamate overactivation while preserving normal synaptic signaling. Targets two distinct mechanisms in Alzheimer's.
Dopamine D2 and serotonin 5-HT2A receptor antagonist'"`UNIQ--ref-0000008D-QINU`"' '"`UNIQ--vote-0000008E-QINU`"'
Dopamine and norepinephrine reuptake inhibitor
Dopamine and serotonin reuptake inhibitor; actoprotector
Dopamine precursor
Dopamine precursor + DOPA decarboxylase inhibitor
Dopamine reuptake inhibitor; tropane analogue
Dual agonist of the [[GIP receptor]] and [[GLP-1 receptor]] ("twincretin").
Endogenous androgen binding to androgen receptors; mediates male secondary sex characteristics, anabolism, libido, erythropoiesis, and CNS effects on mood/energy/aggression. Aromatized peripherally to estradiol; reduced to DHT.
Extremely potent 5-HT2A agonist; vasoconstrictor
Extremely potent 5-HT2A agonist; very long duration
Extremely potent GABAA positive allosteric modulator
Extremely potent mu-opioid receptor agonist
Fluorinated phenibut; GABAB agonist
Full CB1/CB2 agonist
GABA enhancer; sodium channel blocker; histone deacetylase inhibitor
GABA reuptake inhibitor (GAT-1 blocker)
GABA-A positive allosteric modulator'"`UNIQ--ref-00000067-QINU`"' '"`UNIQ--vote-00000068-QINU`"'
GABAA agonist
GABAA modulator; glycine receptor agonist
GABAA modulator; meprobamate prodrug
GABAA positive allosteric modulator; lactate dehydrogenase inhibitor
GABAA positive allosteric modulator; low sedation
GABAA positive allosteric modulator; prodrug of desmethyldiazepam
GABAA positive allosteric modulator; very long half-life
GABAA potentiator
GABAA potentiator; glycine receptor agonist
GABAA potentiator; possible glycine/NMDA modulation
GABAA potentiator; ultra-short-acting
GABAB agonist; GHB receptor agonist
GABAB agonist; alpha-2-delta calcium channel ligand
Glutamate receptor agonist
Glutamate receptor antagonist; GABA modulator
H1 antagonist; muscarinic antagonist
H1 receptor antagonist
High-affinity D2 receptor antagonist
High-affinity choline uptake enhancer
Highest natural caffeine content of any plant (2–7% by dry weight, ~2–4× coffee). Caffeine is bound to tannins, producing a slower release than pure coffee caffeine.
Highly potent mu-opioid receptor agonist
Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol.
Human IgG1 monoclonal antibody targeting aggregated forms of amyloid-β (Aβ), soluble oligomers and insoluble fibrils. Reduces Aβ plaque burden on PET imaging via Fc-mediated microglial clearance. Whether plaque reduction translates to clinical benefit is the core controversy.
Humanized IgG1 monoclonal antibody binding CGRP peptide; IV infusion enables fastest onset of any CGRP mAb
Humanized IgG2 monoclonal antibody binding both isoforms of CGRP peptide
Humanized IgG2 monoclonal antibody binding the CGRP receptor (not the peptide); blocks CGRP-mediated vasodilation and nociceptive signaling
Humanized IgG4 monoclonal antibody binding CGRP peptide; prevents CGRP from activating its receptor
Indirect sympathomimetic; norepinephrine releaser
Irreversible GABA-T inhibitor
Irreversible selective MAO-B inhibitor
Kappa agonist; mu antagonist
Kappa agonist; mu partial agonist
Kappa agonist; mu partial agonist/antagonist
Kappa-opioid agonist; NMDA antagonist; SERT/DAT/NET inhibitor
Kappa-opioid receptor agonist
Kavalactones; GABAA modulator; sigma receptor activity
Local anti-inflammatory; TRPA1 antagonist at therapeutic doses
Long-acting agonist of the [[GLP-1 receptor]].
Long-acting agonist of the [[GLP-1 receptor]]; Fc-fusion construct.
Lysergic acid 2,4-dimethylazetidide; 5-HT2A agonist
Lysergic acid hydroxyethylamide; 5-HT2A agonist
MAO inhibitor; monoamine releasing agent
MAO inhibitor; serotonin releasing agent
MAO-B inhibitor; sodium channel blocker; glutamate release inhibitor
Mechanism incompletely understood
Melatonin receptor agonist
Melatonin receptor agonist; 5-HT2C antagonist
Methaqualone analogue; GABAA potentiator
Mitragynine/7-hydroxymitragynine; mu-opioid partial agonist
Monoamine releasing agent, TAAR1 agonism, VMAT2 substrate, DAT/NET reverse transport
Monoamine releasing agent; 5-HT2A agonist
Monoamine releasing agent; 5-HT2A agonist; MAO inhibitor
Monoamine releasing agent; active ingredient in khat
Monoamine releasing agent; serotonergic at higher doses
Monoamine reuptake inhibitor; sodium channel blocker
Mu-opioid agonist; modulates glutamate AMPA receptors
Mu-opioid agonist; norepinephrine reuptake inhibitor
Mu-opioid receptor agonist; fentanyl analogue
Mu-opioid receptor agonist; prodrug (metabolized to morphine)
Mu-opioid receptor agonist; sodium channel blocker
Mu/delta antagonist; kappa partial agonist
Mu/kappa/delta agonist; NMDA antagonist
Multi-receptor antagonist (D2, 5-HT2A, H1, alpha)
Multiple mechanisms; GPR55 antagonist; TRPV1 agonist
Muscarinic receptor antagonist; dopamine reuptake inhibitor
N-methyl analogue of 2-AI
NMDA antagonist
NMDA antagonist; GABAA modulator
NMDA antagonist; GABAA potentiator
NMDA antagonist; SERT inhibitor; sigma-1 agonist
NMDA antagonist; dopamine releasing agent
NMDA antagonist; endogenous opioid releaser
NMDA antagonist; fluorinated ketamine analogue
NMDA antagonist; kappa-opioid agonist
NMDA antagonist; ketamine analogue
NMDA antagonist; more stimulating than PCP
NMDA antagonist; opioid agonist
NMDA antagonist; potent opioid agonist
NMDA antagonist; sigma receptor agonist
NMDA antagonist; sigma receptor agonist; dopaminergic
NMDA antagonist; sigma-1 agonist; serotonin reuptake inhibitor
NMDA-receptor antagonism
Nicotinic acetylcholine receptor agonist
Non-selective competitive antagonist at β1 and β2 adrenergic receptors. Lipophilic; significant blood–brain barrier penetration, accounting for its CNS effects.
Non-selective dopamine receptor agonist
Norepinephrine and dopamine releasing agent
Norepinephrine releaser
Norepinephrine/dopamine releasing agent
Norepinephrine/dopamine reuptake inhibitor
Norepinephrine–dopamine reuptake inhibition (DAT, NET)
Norepinephrine–dopamine reuptake inhibition (DAT, NET), d-threo enantiomer of methylphenidate
Norepinephrine–dopamine reuptake inhibitor
Once-daily COMT inhibitor
Once-daily agonist of the [[GLP-1 receptor]].
Opioid receptor partial agonist/antagonist; toxic alkaloid
Partial CB1/CB2 agonist
Partial MAOI; anticholinergic effects
Partial agonist at D2 and 5HT1A. Antagonist at 5HT2A, α1A, α1B, α2C. More potent 5HT2A antagonism, 5HT1A partial agonism, and α1 antagonism (relative to D2 partial agonism) than aripiprazole, proposed to reduce akathisia and enhance affective/cognitive effects.
Partial mu-opioid receptor agonist; alpha-2 agonist
Partial nicotinic ACh receptor agonist
Peripheral COMT inhibitor
Phosphodiesterase inhibitor; calcium channel blocker
Positive allosteric modulator of the GABA<sub>A</sub> receptor at the benzodiazepine binding site; increases frequency of Cl<sup>−</sup> channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects.
Potent 5-HT2A agonist; no oral activity
Potent 5-HT2A agonist; sigma-1 agonist
Potent 5-HT2A agonist; very long duration
Potent dopamine and norepinephrine reuptake inhibitor
Potent dopamine/norepinephrine reuptake inhibitor
Potent serotonin reuptake inhibitor; also NRI
Primary alkaloid is (S)-(-)-cathinone, a phenylpropanolamine close kin to amphetamine. Releases dopamine and norepinephrine. Also contains cathine (=norpseudoephedrine) and norephedrine.
Primary alkaloid is arecoline, a muscarinic agonist (M1, M2, M3, M4) and partial agonist at nicotinic receptors. Produces alertness, salivation, sweating, mild euphoria.
Primary alkaloid is cocaine, a tropane that blocks reuptake of dopamine and norepinephrine (and serotonin). At low oral doses from leaf chewing, the slow release favors NE-mediated alertness over DA-mediated euphoria.
Primary alkaloid is theobromine (3,7-dimethylxanthine), with minor caffeine. Also contains phenethylamine, anandamide (an endogenous cannabinoid), tryptophan (serotonin precursor), and flavanols. The combined effect is mild stimulation + mood elevation.
Prodrug of 4-HO-DET; 5-HT2A agonist
Prodrug of 4-HO-DiPT; 5-HT2A agonist
Prodrug of 4-HO-MET; 5-HT2A agonist
Prodrug of 4-HO-MiPT; 5-HT2A agonist
Prodrug of GHB
Prodrug of amphetamine + theophylline
Prodrug of modafinil
Prodrug of morphine; mu-opioid receptor agonist
Prodrug of phenytoin; sodium channel blocker
Prodrug of psilocin; 5-HT2A agonist
Prodrug to [[Psilocin|psilocin]] (4-hydroxy-N,N-dimethyltryptamine), a partial agonist at the [[Receptor:5-HT2A|5-HT2A]] serotonin receptor; the action that defines the classical-psychedelic mechanism
Prodrug; converted to [[Morphine|morphine]] by [[Enzyme:CYP2D6|CYP2D6]] for analgesic action.
R-enantiomer of modafinil; mechanism incompletely understood
Reversible MAO-A inhibitor; NMDA antagonist; beta-carboline
Reversible MAO-A inhibitor; beta-carboline
Reversible inhibitor of MAO-A
Root bark contains ~1% N,N-dimethyltryptamine (DMT) and related tryptamines. Oral activity requires MAOI co-administration.
SV2A ligand (higher affinity than levetiracetam)
Selective GABAA agonist (extrasynaptic delta subunit)
Selective M1 muscarinic antagonist
Selective NET inhibitor (no significant DAT activity, distinguishes from amphetamine/methylphenidate). Also: 5HT1A receptor partial agonism, 5HT2B and 5HT7 receptor antagonism. The serotonergic actions may underlie better tolerability and possibly different efficacy spectrum than atomoxetine.
Selective alpha-1 adrenergic receptor antagonist. Lowers peripheral vascular resistance via vasodilation; in the CNS, blunts noradrenergic hyperarousal thought to drive trauma-related nightmares.
Selective alpha-2A adrenergic receptor agonist
Selective dopamine and norepinephrine reuptake inhibitor (DAT and NET inhibition). Unlike amphetamine, does not significantly release monoamines, pure reuptake inhibition.
Selective inhibitor of PDE5 with a substantially longer half-life than other PDE5 inhibitors, allowing once-daily continuous dosing.
Selective inhibitor of PDE5. Slightly higher PDE5/PDE6 selectivity vs sildenafil (less visual side effect) but more PDE1 cross-activity (occasional QT effects at high doses).
Selective inhibitor of phosphodiesterase type 5 (PDE5), preventing cGMP breakdown in vascular smooth muscle. In the corpus cavernosum, potentiates the NO/cGMP cascade triggered by sexual stimulation.
Selective inhibitor of phosphodiesterase type 5 (PDE5); increases cGMP in cavernous smooth muscle, producing erection in response to sexual stimulation.
Selective inverse agonist at 5HT2A receptors with weaker activity at 5HT2C. Has no significant dopamine D2 affinity, unique among approved antipsychotics. Inverse agonism (rather than antagonism) reduces constitutive 5HT2A receptor activity below baseline.
Selective mu-opioid receptor agonist
Semi-synthetic; CB1 agonist
Serotonin and norepinephrine reuptake inhibitor
Serotonin precursor; 5-hydroxytryptophan
Serotonin releaser; sigma-1 agonist
Serotonin releasing agent
Serotonin releasing agent; 5-HT2A agonist
Serotonin releasing agent; monoamine reuptake inhibitor
Serotonin reuptake inhibitor and 5-HT2A antagonist
Serotonin/dopamine/norepinephrine releasing agent; 5-HT2A agonist
Serotonin/norepinephrine/dopamine releasing agent
Serotonin–norepinephrine reuptake inhibition (balanced)
Serotonin–norepinephrine reuptake inhibitor
Slow-inactivation sodium channel enhancer; CRMP-2 ligand
Small-molecule CGRP receptor antagonist; intranasal formulation
Sodium channel blocker; GABAA positive allosteric modulator
Sodium channel modulator
Sodium/T-type calcium channel blocker; carbonic anhydrase inhibitor
Source of DMT-class tryptamines
Source of [[DMT]], bufotenine, and 5-MeO-DMT
Source of [[DMT|N,N-dimethyltryptamine]]
Synthetic T4 (thyroxine); peripherally deiodinated to T3 (triiodothyronine), the active hormone. '"`UNIQ--vote-00000031-QINU`"' Narrow therapeutic index; brand-to-generic switches can shift TSH and require re-titration'"`UNIQ--ref-00000032-QINU`"'.
Synthetic THC; CB1/CB2 agonist
Synthetic cannabinoid; CB1/CB2 agonist
Synthetic neuroactive steroid (an analog of allopregnanolone), bioavailable orally unlike brexanolone. Positive allosteric modulator at GABA-A receptors including extrasynaptic δ-containing subtypes.
T-type calcium channel blocker
TAAR1 agonism, VMAT2 substrate, DAT/NET reverse transport, net release of dopamine and norepinephrine
THC + CBD; CB1/CB2 agonist
The d-enantiomer is a highly β1-selective antagonist; the l-enantiomer triggers endothelial nitric-oxide–mediated vasodilation. Unique among beta blockers for this NO mechanism.
Thioxanthene D2 antagonist
Trace amine-associated receptor 1 (TAAR1) agonist; monoamine releaser
TrkB/BDNF'"`UNIQ--ref-00000047-QINU`"' '"`UNIQ--vote-00000048-QINU`"'
TrkB/BDNF'"`UNIQ--ref-00000084-QINU`"' '"`UNIQ--vote-00000085-QINU`"'
Tropane alkaloids: hyoscyamine (dominant; the racemic form is atropine), scopolamine. Competitive muscarinic antagonism.
Tropane alkaloids: hyoscyamine, scopolamine, atropine, apoatropine.
Tropane alkaloids: hyoscyamine, scopolamine, in higher seed concentrations than belladonna or datura.
Tropane alkaloids: scopolamine (dominant), hyoscyamine, atropine. Competitive antagonism at muscarinic acetylcholine receptors.
Ultra-short-acting mu-opioid agonist
Very potent 5-HT2A agonist; long duration
Weak CB1 partial agonist; weak CB2 partial agonist; multiple secondary targets.
Weak SRI; primarily H1/D2/alpha antagonist
Weak partial agonist at CB1 and CB2; alpha-2 adrenergic agonist; 5-HT1A antagonist; multiple TRP channel effects.
Weak serotonin reuptake inhibitor; beta-carboline
'"`UNIQ--vote-00000013-QINU`"' Anticholinergic burden (dry mouth, blurred vision, urinary retention, cognitive effects) is the principal adverse-event concern and the basis for Beers-list cautions in elderly patients'"`UNIQ--ref-00000014-QINU`"'.
'"`UNIQ--vote-00000013-QINU`"' Does not stimulate insulin secretion; minimal hypoglycemia risk as monotherapy. Cleared renally unchanged; dose-adjust by eGFR'"`UNIQ--ref-00000014-QINU`"'. Rare lactic acidosis primarily in renal failure or acute illness.
'"`UNIQ--vote-00000013-QINU`"' Once converted, dextroamphetamine acts by displacing dopamine and norepinephrine from presynaptic vesicles via VMAT-2 and reversing DAT and NET transport, the shared mechanism of all amphetamine-class agents'"`UNIQ--ref-00000014-QINU`"'.
'"`UNIQ--vote-00000013-QINU`"' Strong CYP3A4 induction via the phenobarbital metabolite produces many interactions (reduces oral contraceptives, warfarin, many psychotropics). Essential-tremor efficacy is the unique pharmacological selling point'"`UNIQ--ref-00000014-QINU`"'.
'"`UNIQ--vote-00000015-QINU`"' CYP2D6 metabolism produces stereoselective clearance; CYP2D6 poor metabolizers have higher plasma exposure and may need lower doses'"`UNIQ--ref-00000016-QINU`"'.
'"`UNIQ--vote-00000015-QINU`"' Pediatric ingestion (capsule chewed or punctured) releases the free local anesthetic and causes seizures, cardiac arrhythmia, and death'"`UNIQ--ref-00000016-QINU`"'.
'"`UNIQ--vote-00000015-QINU`"' The favorable pregnancy safety profile and the dual mechanism support its first-line role in pregnancy-associated hypertension and in hypertensive emergencies where rapid, controllable BP reduction is needed'"`UNIQ--ref-00000016-QINU`"'.
'"`UNIQ--vote-00000016-QINU`"' Bicarbonate is not benign: high-volume use produces hypernatremia, metabolic alkalosis, hypokalemia, and (in arrest) paradoxical intracellular acidosis'"`UNIQ--ref-00000017-QINU`"'.
'"`UNIQ--vote-00000016-QINU`"' Brand-to-brand and lot-to-lot variability in T3:T4 ratio is greater than with synthetic levothyroxine, which is why endocrine guidelines prefer the synthetic'"`UNIQ--ref-00000017-QINU`"'.
'"`UNIQ--vote-00000017-QINU`"' Anticholinergic and sedating, with the standard first-generation antihistamine Beers-list concerns in elderly patients'"`UNIQ--ref-00000018-QINU`"'.
'"`UNIQ--vote-00000019-QINU`"' Once-daily dosing is a clinical advantage over short-half-life NSAIDs'"`UNIQ--ref-0000001A-QINU`"'.
'"`UNIQ--vote-00000019-QINU`"' Sedation and hypotension are the dose-limiting effects; gradual titration and bedtime or split dosing mitigate both. Abrupt discontinuation can precipitate rebound hypertension, particularly with long-standing use'"`UNIQ--ref-0000001A-QINU`"'.
'"`UNIQ--vote-00000019-QINU`"' Therapeutic plasma-level monitoring is standard practice for TCAs given the narrow therapeutic index and the established plasma-level-efficacy correlation. CYP2D6 substrate; CPIC PGx guidance applies for dose individualization'"`UNIQ--ref-0000001A-QINU`"'.
'"`UNIQ--vote-0000001B-QINU`"' '''Priapism''' is a recognized rare adverse effect via α1 antagonism in penile vasculature and is the marquee counseling point for male patients'"`UNIQ--ref-0000001C-QINU`"'.
'"`UNIQ--vote-0000001D-QINU`"' '''QT prolongation''' risk at high doses prompted the FDA's 2015 caution against use in patients with prolonged QT or with concurrent QT-prolonging medicines'"`UNIQ--ref-0000001E-QINU`"'.
'"`UNIQ--vote-0000001D-QINU`"' CYP2C19 + CYP3A4 metabolism, with CPIC PGx guidance: poor CYP2C19 metabolizers have ~3-fold higher exposure and benefit from a lower starting dose; ultrarapid metabolizers may have inadequate response'"`UNIQ--ref-0000001E-QINU`"'.
'"`UNIQ--vote-0000001D-QINU`"' Major Beers-list concern in elderly patients for cognitive and fall risks. CYP2D6 substrate. At massive overdose, also produces sodium channel blockade with cardiac toxicity'"`UNIQ--ref-0000001E-QINU`"'. '"`UNIQ--effect-0000001F-QINU`"'
'"`UNIQ--vote-00000037-QINU`"' Hypertonic 3% is the standard urgent treatment of severely symptomatic hyponatremia'"`UNIQ--ref-00000038-QINU`"'.
'"`UNIQ--vote-00000049-QINU`"'
'"`UNIQ--vote-0000004E-QINU`"' The EPA+DHA mix is biochemically and clinically distinct from icosapent ethyl'"`UNIQ--ref-0000004F-QINU`"'.
'"`UNIQ--vote-00000053-QINU`"' Also raises bradykinin, contributing to vasodilation and the characteristic dry cough. Renally cleared, unmetabolized; dose-adjust by eGFR'"`UNIQ--ref-00000054-QINU`"'.
'"`UNIQ--vote-00000054-QINU`"' The clinical efficacy endpoint is adequate visualization at colonoscopy, scored by the Boston Bowel Preparation Scale'"`UNIQ--ref-00000055-QINU`"'.
'"`UNIQ--vote-00000073-QINU`"' The long half-life gives smooth, once-daily BP control with low rebound. CYP3A4 substrate; pedal edema is the characteristic, dose-related, non-fluid-overload side effect'"`UNIQ--ref-00000074-QINU`"'.
'"`UNIQ--vote-00000086-QINU`"' Calcium content is a relative contraindication for co-administration with citrated blood products through the same line'"`UNIQ--ref-00000087-QINU`"'.
'"`UNIQ--vote-00000093-QINU`"' At higher doses β2 selectivity is lost, producing β1 effects (tachycardia, tremor) and hypokalemia from intracellular potassium shift'"`UNIQ--ref-00000094-QINU`"'.
'"`UNIQ--vote-000000B6-QINU`"' Active metabolite EXP3174 is ~10-40-fold more potent than the parent and accounts for most of the antihypertensive effect; CYP2C9 polymorphism affects conversion'"`UNIQ--ref-000000B7-QINU`"'.
'"`UNIQ--vote-000000D8-QINU`"' Recovery of acid output requires synthesis of new pump enzyme. CYP2C19 substrate; PGx genotype substantially affects exposure and efficacy'"`UNIQ--ref-000000D9-QINU`"'.
'"`UNIQ--vote-000000F7-QINU`"' Minimal CYP3A4 dependence (CYP2C9 minor) reduces drug-drug interactions; transport in and out of hepatocytes is largely via OATP1B1, making SLCO1B1 PGx genotype the most clinically actionable marker for statin-associated myopathy'"`UNIQ--ref-000000F8-QINU`"'.
'"`UNIQ--vote-00000117-QINU`"' Compared with omeprazole, pantoprazole has a more linear pharmacokinetic profile and is metabolized predominantly via CYP2C19 with CYP3A4 contribution; less CYP2C19-driven drug interaction with clopidogrel than omeprazole'"`UNIQ--ref-00000118-QINU`"'.
'"`UNIQ--vote-00000138-QINU`"' Decreases urinary calcium (used in stone prevention); raises serum uric acid, glucose, and lipids modestly; non-anion-gap hypokalemic metabolic alkalosis is the characteristic electrolyte pattern'"`UNIQ--ref-00000139-QINU`"'.
'"`UNIQ--vote-00000199-QINU`"' Extends ampicillin's spectrum with better oral bioavailability. Susceptible to β-lactamases; clavulanate co-administration restores activity against many resistant organisms'"`UNIQ--ref-0000019A-QINU`"'.
'"`UNIQ--vote-000001F6-QINU`"' CYP3A4 (primary) and P-glycoprotein substrate; strong dual inhibitors or inducers materially shift exposure. Reversal: andexanet alfa for life-threatening bleeding; 4F-PCC commonly used off-label when andexanet unavailable'"`UNIQ--ref-000001F7-QINU`"'.
'"`UNIQ--vote-00000237-QINU`"' Binds the same insulin receptor as endogenous insulin with comparable mitogenic-to-metabolic ratio; provides basal hepatic glucose suppression and peripheral glucose uptake without prandial peaks'"`UNIQ--ref-00000238-QINU`"'.
'"`UNIQ--vote-00000255-QINU`"' Less potent and shorter-acting than PPIs but with faster on-effect; suitable for on-demand acid suppression. Largely renally cleared; dose-adjust in renal impairment to avoid CNS effects (confusion in elderly)'"`UNIQ--ref-00000256-QINU`"'.
'"`UNIQ--vote-000002D7-QINU`"' Hypoglycemia is the central risk, especially in elderly and renally impaired patients (glipizide has shorter half-life than glyburide, which is one reason it is preferred in older adults). CYP2C9 substrate; weight gain typical.
'"`UNIQ--vote-0000032A-QINU`"' D3 (cholecalciferol) is more potent at raising serum 25(OH)D per dose; D2 remains widely prescribed in the US Rx 50,000 IU formulation'"`UNIQ--ref-0000032B-QINU`"'.
'"`UNIQ--vote-00000391-QINU`"' Minimal CYP metabolism; mostly renally cleared unchanged. Cetirizine is the active racemate; levocetirizine is the active R-enantiomer marketed separately'"`UNIQ--ref-00000392-QINU`"'.
'"`UNIQ--vote-000003D1-QINU`"' SLCO1B1 polymorphism affects exposure but is most clinically actionable for simvastatin'"`UNIQ--ref-000003D2-QINU`"'.
'"`UNIQ--vote-0000042C-QINU`"' D3 is more potent than D2 at raising and sustaining serum 25(OH)D per dose, and is the more common OTC formulation; D2 remains the dominant Rx 50,000 IU formulation in the US for historical reasons.
'"`UNIQ--vote-000004A9-QINU`"' Modest HDL rise; LDL effects mixed. Renally cleared; combination with statin carries elevated myopathy risk (greater for gemfibrozil than fenofibrate, but caution still warranted)'"`UNIQ--ref-000004AA-QINU`"'.
'"`UNIQ--vote-000004C8-QINU`"' Largely hepatically cleared (~80% biliary); no active metabolite. Sacubitril-valsartan (Entresto) combines an ARB with neprilysin inhibition for HFrEF and was a notable advance over the ARB-alone trial (PARADIGM-HF, 2014)'"`UNIQ--ref-000004C9-QINU`"'.
'"`UNIQ--vote-0000050D-QINU`"' CYP3A4 (primary) and P-glycoprotein substrate; strong dual inhibitors or inducers materially shift exposure. Reversal: andexanet alfa for life-threatening bleeding; 4F-PCC commonly used off-label when andexanet unavailable'"`UNIQ--ref-0000050E-QINU`"'.
'"`UNIQ--vote-00000584-QINU`"' Binds the same insulin receptor as endogenous insulin with comparable mitogenic-to-metabolic ratio. Ultra-rapid formulations (Lyumjev) add treprostinil and citrate to accelerate absorption further'"`UNIQ--ref-00000585-QINU`"'.
'"`UNIQ--vote-000005D0-QINU`"' Selectivity comes from the viral-kinase-only initial phosphorylation step, which is why uninfected cells generate minimal active drug'"`UNIQ--ref-000005D1-QINU`"'. Dose-adjust by renal function; rare crystalline nephropathy with rapid IV acyclovir.
'"`UNIQ--vote-0000061E-QINU`"' Less reliably anticholinergic than first-generation H1s; minimal antiemetic effect. Desloratadine (Clarinex) is the active enantiomer-of-metabolite version marketed as a Rx alternative.
'"`UNIQ--vote-0000063C-QINU`"' Avoid in HFrEF (negative inotropy). CYP3A4 substrate AND moderate inhibitor — interacts substantially with statins (especially simvastatin), tacrolimus, cyclosporine, and many other CYP3A4 substrates'"`UNIQ--ref-0000063D-QINU`"'.
'"`UNIQ--vote-000006BE-QINU`"' Drug-holiday concept (3-5 years on, 1-2 years off) emerged from FLEX and long-term safety data balancing fracture protection against atypical femoral fracture and osteonecrosis of the jaw signals'"`UNIQ--ref-000006BF-QINU`"'.
'"`UNIQ--vote-00000762-QINU`"' Largely renally cleared, hence the eGFR-tiered dosing. Rare but well-documented signals: acute pancreatitis (uncertain causal contribution), severe joint pain, and bullous pemphigoid (class effect, especially in older Asian patients)'"`UNIQ--ref-00000763-QINU`"'.
'"`UNIQ--vote-0000083E-QINU`"' CYP2C9 substrate; no clinically active metabolites. The IDNT trial established renoprotection in diabetic nephropathy independent of BP lowering, contributing to the ARB class indication in T2DM with proteinuria'"`UNIQ--ref-0000083F-QINU`"'.
'"`UNIQ--vote-00000860-QINU`"' Activates the glucocorticoid receptor to broadly remodel inflammatory, immune, and metabolic transcription. Unlike prednisone, it does not require hepatic activation, making it the preferred oral choice in severe hepatic dysfunction'"`UNIQ--ref-00000861-QINU`"'.
'"`UNIQ--vote-000008BE-QINU`"' Preferred over prednisone in advanced hepatic dysfunction where hepatic 11β-HSD1 activation is impaired. Liquid formulations are the workhorse pediatric oral corticosteroid for asthma and croup'"`UNIQ--ref-000008BF-QINU`"'.
'"`UNIQ--vote-000008E1-QINU`"' Like omeprazole, it is an acid-activated prodrug that covalently and irreversibly binds the H+/K+ ATPase. CYP2C19 PGx remains clinically relevant for both'"`UNIQ--ref-000008E2-QINU`"'.
'"`UNIQ--vote-00000950-QINU`"' Mostly renally cleared unchanged; dose-reduce in renal impairment. Like cetirizine, retains slightly more sedation than fexofenadine in some users'"`UNIQ--ref-00000951-QINU`"'.
'"`UNIQ--vote-00000975-QINU`"' Hyperammonemic encephalopathy (consider in any unexplained CNS depression), thrombocytopenia, and polycystic ovary syndrome are characteristic chronic-use adverse effects beyond hepatic and pancreatic risks'"`UNIQ--ref-00000976-QINU`"'.
'"`UNIQ--vote-000009FD-QINU`"' Active against gram-positive cocci including MRSA; the unique target underlies the absence of cross-resistance with other antibiotic classes. High-level resistance (plasmid-mediated mupA) is rising and limits prolonged or repeated use'"`UNIQ--ref-000009FE-QINU`"'.
'"`UNIQ--vote-00000A1D-QINU`"' Like other ACE inhibitors, it raises bradykinin (driving the dry cough and rare angioedema). Renally cleared; dose-adjust in renal impairment'"`UNIQ--ref-00000A1E-QINU`"'.
'"`UNIQ--vote-00000AEA-QINU`"' The 24-hour half-life supports once-daily dosing with consistent overnight BP control. Largely hepatically cleared (~98% biliary); no significant renal clearance dependence'"`UNIQ--ref-00000AEB-QINU`"'.
'"`UNIQ--vote-00000B40-QINU`"' The TRANSFORM-HF trial (2023) found no all-cause mortality difference between torsemide and furosemide in heart failure, although torsemide remains pharmacologically preferred where furosemide oral absorption is unreliable'"`UNIQ--ref-00000B41-QINU`"'.
'"`UNIQ--vote-00000CC9-QINU`"' Mostly excreted unchanged in feces and urine; P-glycoprotein substrate (the basis of the fruit-juice interaction).
'"`UNIQ--vote-00000D11-QINU`"' Same mechanistic family as amphotericin B but with prohibitive systemic toxicity at therapeutic doses, hence restriction to topical and luminal-gut indications. No clinically meaningful resistance after decades of use'"`UNIQ--ref-00000D12-QINU`"'.
'"`UNIQ--vote-00000D7A-QINU`"' Substantial QT-interval prolongation — the most QT-prolonging fluoroquinolone — limits use in patients on other QT-prolonging agents or with electrolyte abnormalities'"`UNIQ--ref-00000D7B-QINU`"'.
'"`UNIQ--vote-00000DFA-QINU`"' CYP3A4 substrate; QT-interval prolongation has been reported at higher doses. Like other antimuscarinics, contributes to cumulative anticholinergic burden in older adults'"`UNIQ--ref-00000DFB-QINU`"'.
'"`UNIQ--vote-00000E4A-QINU`"' The narrow safe-bolus window for IV use (sharp risk of arrhythmia, hypertensive emergency, intracerebral hemorrhage) is why anaphylaxis dosing is '''IM, not IV''', outside critical care'"`UNIQ--ref-00000E4B-QINU`"'.
'"`UNIQ--vote-00000ECD-QINU`"' Agranulocytosis is the most-feared adverse effect (~0.3%, usually first 90 days of treatment; warn patients to seek urgent CBC for fever or severe sore throat). Hepatotoxicity is class-recognized but more often associated with PTU'"`UNIQ--ref-00000ECE-QINU`"'.
'"`UNIQ--vote-00001014-QINU`"' Activates the glucocorticoid receptor to broadly remodel inflammatory, immune, and metabolic transcription. The dipropionate, valerate, and augmented dipropionate ester forms determine topical potency (high to super-high)'"`UNIQ--ref-00001015-QINU`"'.
'"`UNIQ--vote-0000104D-QINU`"' Adequate hydration is at least as important as the drug in producing the expectorant effect clinically. Used in combination with dextromethorphan, decongestants, or antihistamines in many proprietary OTC cold preparations.
'"`UNIQ--vote-00001067-QINU`"' Chronic use is associated with cathartic colon (colonic dilation, loss of haustration), hypokalemia, and laxative dependence; reserved for short-term use or bowel prep with breaks between courses'"`UNIQ--ref-00001068-QINU`"'.
'"`UNIQ--vote-000010F8-QINU`"' Pre-treatment screening for latent TB (PPD or IGRA) and chronic hepatitis B is standard. Anti-drug antibody formation is a recognized cause of secondary loss of response'"`UNIQ--ref-000010F9-QINU`"'.
'"`UNIQ--vote-0000111B-QINU`"' Intraoperative floppy iris syndrome is a recognized class effect. Recently emerging evidence (observational) suggests possible Parkinson's disease risk reduction via PGK1 binding — investigational and not a clinical indication'"`UNIQ--ref-0000111C-QINU`"'.
'"`UNIQ--vote-0000113A-QINU`"' Concomitant β-blocker or CCB is required when used for AF to prevent 1:1 atrial flutter conduction (flecainide can slow atrial rate to a level where AV conduction allows dangerous ventricular rates). CYP2D6 substrate'"`UNIQ--ref-0000113B-QINU`"'.
'"`UNIQ--vote-00001197-QINU`"' Extracellular cGMP separately activates submucosal sensory afferents in a way that reduces visceral pain perception, distinguishing linaclotide from purely osmotic laxatives in IBS-C. Diarrhea is the dose-limiting effect'"`UNIQ--ref-00001198-QINU`"'.
'"`UNIQ--vote-000011D5-QINU`"' Minimal systemic absorption and the dual mechanism underlie its first-line role in seasonal allergic conjunctivitis. Comfort drops without preservatives are available for sensitive patients'"`UNIQ--ref-000011D6-QINU`"'.
'"`UNIQ--vote-000011F4-QINU`"' Like all NSAIDs, raises CV thrombotic risk modestly (FDA 2014/2015 advisory) and produces GI, renal, hypertensive, and platelet-inhibitory effects characteristic of the class'"`UNIQ--ref-000011F5-QINU`"'.
'"`UNIQ--vote-00001233-QINU`"' Onychomycosis cure rates with nail lacquer are modest (mycologic cure ~30-50%, complete cure ~5-12% at 48 weeks); oral terbinafine remains substantially more effective when systemic therapy is acceptable'"`UNIQ--ref-00001234-QINU`"'.
'"`UNIQ--vote-0000124C-QINU`"' The 400 mg/d dose for migraine prophylaxis is supported by randomized trials (Schoenen 1998) and remains a low-risk evidence-based supplement option. Characteristic bright-yellow urine fluorescence with high-dose oral supplementation.
'"`UNIQ--vote-00001269-QINU`"' Renal, GI, hypertensive, and CV effects parallel the class profile; modest COX-2 preference may underlie some literature suggesting slightly better GI tolerability than non-selective NSAIDs, though clinically the difference is small'"`UNIQ--ref-0000126A-QINU`"'.
'"`UNIQ--vote-00001284-QINU`"' Systemic oral ketotifen (available outside US) has historical use for asthma adjunct therapy via the same dual mechanism, but oral use produces sedation and weight gain — the topical ophthalmic application largely avoids both'"`UNIQ--ref-00001285-QINU`"'.
'"`UNIQ--vote-00001302-QINU`"' Renally cleared; accumulation in advanced CKD can produce neuromuscular and cardiac depression. Hypomagnesemia frequently co-exists with hypokalemia and is often the reason refractory potassium loss does not correct until magnesium is repleted.
'"`UNIQ--vote-0000132D-QINU`"' Electrolyte-balanced bowel-prep formulations are designed to be iso-osmotic with plasma so the volume passes through without net fluid or electrolyte shifts, the basis of their safety for whole-bowel evacuation.
'"`UNIQ--vote-00001356-QINU`"' Binds the same insulin receptor as endogenous insulin with comparable mitogenic-to-metabolic ratio'"`UNIQ--ref-00001357-QINU`"'.
'"`UNIQ--vote-000013B1-QINU`"' Topical application minimizes systemic antihistaminic burden; the characteristic bitter taste with nasal use (drainage to oropharynx) is the main tolerability issue'"`UNIQ--ref-000013B2-QINU`"'.
'"`UNIQ--vote-000013EE-QINU`"' Higher-dose Aygestin (5 mg) achieves more reliable ovulation suppression and is used for endometriosis and DUB. POP requires strict daily timing because the 24-hour cervical-mucus effect window is narrower than COC'"`UNIQ--ref-000013EF-QINU`"'.
'"`UNIQ--vote-000014BC-QINU`"' Topical ophthalmic and otic formulations remain widely used in ENT and ophthalmology. Subject to all fluoroquinolone-class restrictions (tendinitis/rupture, peripheral neuropathy, QT prolongation)'"`UNIQ--ref-000014BD-QINU`"'.
'"`UNIQ--vote-000014DD-QINU`"' The combination is the most-prescribed opioid analgesic in the US for moderate-to-severe acute pain. CPIC PGx guidance addresses CYP2D6-driven exposure variation'"`UNIQ--ref-000014DE-QINU`"'.
'"`UNIQ--vote-000014F7-QINU`"' Falling out of favor for acute pain due to aspirin's GI bleeding and antiplatelet effects compared with acetaminophen-opioid combinations; still used in selected indications'"`UNIQ--ref-000014F8-QINU`"'.
'"`UNIQ--vote-00001513-QINU`"' The combination with acetaminophen provides additive non-opioid analgesia and lowers required codeine dose. CYP2D6 PGx is one of the most clinically actionable in current pharmacology; CPIC supports genotype-guided opioid selection'"`UNIQ--ref-00001514-QINU`"'.
'"`UNIQ--vote-00001549-QINU`"' Metabolic effects (weight gain, dyslipidemia, glucose dysregulation) dominate the long-term tolerability profile; routine metabolic monitoring is standard'"`UNIQ--ref-0000154A-QINU`"'.
'"`UNIQ--vote-00001580-QINU`"' First FDA-approved treatment for PBA. The 10 mg quinidine daily dose is far below antiarrhythmic levels but sufficient to nearly fully inhibit CYP2D6, the basis of the combination's pharmacokinetic rationale'"`UNIQ--ref-00001581-QINU`"'.
'"`UNIQ--vote-000015CE-QINU`"' The dual-mechanism design exploits the inflammatory component of migraine that triptan monotherapy does not fully address. Risk of serotonin syndrome with SSRIs/SNRIs is theoretical but generally not seen clinically at triptan doses'"`UNIQ--ref-000015CF-QINU`"'.
µ-opioid agonism
Search
uses:
'"`UNIQ--vote-00000FB3-QINU`"', '''adjunctive only''' (does not treat the underlying infection) (1)
starting dose:
100-200 mg PO TID after meals × no more than 2 days when used with concurrent antibiotic (1)
preparations:
95 mg (OTC), 99.5 mg, 100 mg, 200 mg tablets (1)
fda max:
Limit to 48 hours of use to avoid hemolysis and methemoglobinemia (1)
routes:
Oral (1)
onset:
(Click arrow to add another value)
None
·
Hours
·
30-60 minutes
·
1-2 hours
·
~30 min
·
LDL lowering at 2 weeks, max by 4 weeks
·
~1 hour
·
15-30 minutes
·
15–30 min
·
1–2 h
·
30–60 min
·
Antidepressant effect emerges over 1-2 weeks
·
BP and symptomatic LUTS improvement within 1-2 weeks
·
BP effect within 1-2 weeks
·
Clinical improvement within 24-72 hours
·
Days
·
Motor improvement over days at therapeutic dose
·
Over weeks
·
Postprandial glucose effect within days; HbA1c by 12 weeks
·
Sleep effect from first dose; antidepressant effect over 1-4 weeks
Other values:
'''Anxiolytic effect emerges over 2-4 weeks'''; buspirone does NOT work for acute anxiety, which is the central teaching point and the most common cause of treatment failure
1 hour PO; minutes IV
1-2 hours (oral)
1-2 hours (slower than immediate-release amphetamine because activation requires enzymatic cleavage in red blood cells)
1-2 hours PO
1-2 hours for migraine relief
1-2 weeks for antidepressant effect; smoking-cessation effect builds over the first 1-2 weeks
1-2 weeks for neuropathic pain and anxiolytic effect; anticonvulsant effect at therapeutic plasma level
1-3 days
1-3 hours (slower onset than cetirizine; symptom relief somewhat less)
10 minutes (SC); 15-30 minutes (nasal); 30-60 minutes (oral)
10-30 minutes
10-30 minutes (IR)
15 minutes
15-20 minutes
15-30 minutes (oral)
15-30 minutes (oral); 1-2 minutes (IV)
15-60 minutes (oral); 1-5 minutes (IV); 4-10 minutes (rectal or intranasal)
15–30 min (fasting)
1–2 h (PO), immediate (IV)
1–2 h (PO); immediate (IV)
1–2 weeks for muscle effects; preventive migraine benefit accrues over 12-week cycles
2-3 hours per dose; full acid suppression after 3-5 days
20 minutes (oral); 5 minutes (IV)
20-45 min subjective onset; psilocin formation from psilocybin requires intestinal and hepatic alkaline phosphatase
20-60 minutes
20–60 min (oral)
30 min
30 minutes
30 minutes (IM); 30-60 minutes (oral)
30 minutes PO; minutes IV
30 minutes for migraine relief
30-60 min (IR oral); 2-3 days to steady state (transdermal patch)
30-60 min (immediate-release); 1-2 h (extended-release)
30-60 min (sedation); days to weeks (neuroleptic effect)
30-60 minutes (IR)
30-60 minutes (PO)
30-60 minutes (immediate-release oral)
30-60 minutes (oral)
30-60 minutes (oral); 5 minutes (IV); 15-30 minutes (IM)
30-60 minutes (oral); rapid relief in acute gout
30-60 minutes (oral); slower for topical
30–60 min (PO)
30–60 min (SL)
30–60 minutes
30–90 min
4-6 weeks for full antidepressant effect (claimed earlier onset for some patients due to 5HT1A partial agonism)
45-75 min (oral)
5-10 minutes (IV); 30 minutes (oral IR); slower for ER and rectal
<1 minute (IV); 1-2 minutes (infiltration); 30+ minutes (patch on adult skin, faster on thinner pediatric skin)
ADHD effect emerges over 1-2 weeks (slower than psychostimulants); full effect 4-6 weeks
ADHD symptom improvement reported within 1-2 weeks (faster than atomoxetine which takes 4-6 weeks)
AF conversion within hours of single PO dose
Acid suppression within hours; full effect after 3-5 days of dosing
Acute: minutes (IV); chronic: bone effect over months
Amyloid PET clearance within months; cognitive benefit over 18 months
Analgesia within 30 minutes; full anti-inflammatory effect over days
Analgesia within hours; anti-inflammatory effect over days
Analgesic effect within hours; full anti-inflammatory effect over 1-2 weeks
Anti-inflammatory effect within 24 hours of gout flare onset; loses effectiveness if delayed
Anticoagulant effect at 24-72 hours; full INR effect 5-7 days
Anticonvulsant effect emerges with slow titration over weeks; tremor effect over weeks
Anticonvulsant effect within days at therapeutic level; migraine prophylaxis effect emerges over 2-3 months
Anticonvulsant effect within days at therapeutic plasma level
Anticonvulsant effect within days at therapeutic plasma level; rapid titration possible
Anticonvulsant effect within days; mood-stabilizing effect 1-3 weeks
Anticonvulsant effect within days; trigeminal neuralgia relief 24-72 hours; mood-stabilizing effect over weeks
Antidepressant effect emerges over 1-2 weeks; full clinical effect 4-6 weeks
Antidepressant effect over 1-2 weeks; anxiolytic effect over 4-6 weeks
Antidepressant effect over 1-2 weeks; full clinical effect 4-6 weeks
Antidepressant effect within hours of infusion start; sustained at 30 days
Antiepileptic effect within days at therapeutic level; mood-stabilizing effect emerges over weeks
Antihypertensive effect within 1 week; heart-failure mortality benefit accrues over months of titration
Antimanic effects begin within 5-7 days of reaching therapeutic serum levels, with full response often requiring 2-3 weeks. For acute mania, a neuroleptic is typically added for rapid sedation while lithium takes effect.'"`UNIQ--ref-00000053-QINU`"'
Antiplatelet effect within 2 hours of a loading dose; steady-state at 5-7 days of maintenance dosing
Antiplatelet effect within 30 minutes of loading dose (faster than clopidogrel)
Antiplatelet effect within 30-60 minutes; analgesic effect 30-60 minutes
Antipsychotic effect over weeks
Anxiolysis classically 3-4 weeks, continuing improvement to 8-12 weeks
Appetite suppression within hours; weight loss over weeks-months
BP effect 1 hour; max at 4-6 hours
BP effect 1-2 hours; max at 6 hours
BP effect 1-2 weeks; antihypertensive peak 3-6 weeks
BP effect 1-2 weeks; max at 2-3 weeks
BP effect 2 hours; max at 4-6 weeks
BP effect within 24 hours; full effect at 1-2 weeks (long half-life)
BP effect within hours (oral); 5-10 minutes (IV)
BP effect within hours (oral); IOP reduction within 30 minutes, full effect 1-2 weeks (ophthalmic)
BP effect within hours; full effect over 1-2 weeks
BP lowering within 1 hour; max at 6 hours
BP lowering within 1 hour; max effect at 6 hours
BPH symptom improvement at 3-6 months; prostate volume reduction over 6-12 months; hair regrowth at 6-12 months
Benefit over weeks of dosing
Biochemical improvement within 2-4 weeks; full euthyroid state 6-12 weeks
Bone marker reduction within weeks; BMD improvement at 1-3 years; fracture-risk reduction documented at 3-5 years
Bowel movement within 1 week; abdominal pain improvement over weeks
Bronchodilation 15-30 minutes
Bronchodilation 30 minutes; steady-state at 1-2 weeks
Bronchodilation within 1-2 hours; full controller effect 1-2 weeks
Caries reduction over months to years of consistent use
Clinical and mycologic cure follows the full course; nail clearance over months of regrowth
Cognitive effect emerges gradually over weeks to months; ceiling effect at the therapeutic dose
Cognitive effect emerges gradually over weeks to months; symptomatic effect only
Component effects accumulate over weeks
Constipation: 1-3 days; bowel prep: 1-3 hours after starting
Constipation: 24-48 hours; HE: ammonia reduction within hours of stool production
Contraception within 48 hours of starting (POP); endometrial effects days
Contraceptive within 24 hours if given in first 5 days of cycle; otherwise backup for 7 days
Day 3 of dosing in trials; sustained through day 45
Days for calcium effect; weeks for PTH suppression
Days for dermatophyte clearance; nail clearance over months
Days for immunosuppressive effect
Days for symptom improvement in scurvy
Days to weeks for tissue saturation
Days to weeks to raise 25(OH)D; clinical effect on bone over months
Diuresis at 2 hours; antihypertensive effect within days, max at 3-4 weeks
Diuresis at 2-3 hours; BP effect over weeks
Effect demonstrated within 24 hours in some patients
Effects accumulate over weeks; assess at 8 weeks
Estrogen suppression within days; clinical effect over months
First bowel movement within 1-2 hours
Glucose lowering within days; HbA1c effect at 8-12 weeks
Glycemic effect within days; full weight effect over months'"`UNIQ--ref-00000301-QINU`"'
Glycemic effect within days; near-maximal HbA1c effect by 4 weeks at any given dose'"`UNIQ--ref-00000057-QINU`"'
Glycemic effect within days; weight effect over weeks to months'"`UNIQ--ref-00000188-QINU`"'
Glycemic effect within days;<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> full weight effect over months'"`UNIQ--ref-00000250-QINU`"'
Glycemic effect within hours (Byetta); weeks (Bydureon, extended-release microsphere)'"`UNIQ--ref-000000EA-QINU`"'
Glycosuria within hours; HbA1c effect at 12 weeks; CV/renal benefits over months
Glycosuria within hours; HbA1c effect at 12 weeks; cardiovascular and renal benefits over months
Gradual; full clinical effect over 2-4 weeks of titration
HbA1c effect at 12-16 weeks (slower than other classes)
Headache relief at 30-60 minutes
Hematologic response within days
Hours (PO); IV faster but rate-limited
Hours (faster than T4); peak biologic activity 24-48 hours
Hours (systemic); minutes (ophthalmic)
Hours (transdermal); days (IM esters)
Hours to days
Hours to days for inflammation; substantial improvement within 1 week
IM: 5-10 minutes; IV: seconds; nebulized: 5-10 minutes
IOP lowering at 1 hour; max at 2-3 hours
IOP lowering at 2 hours; max at 4 hours
IOP lowering at 3-4 hours; maximum at 8-12 hours
IOP lowering at 4 hours, maximum at 8-12 hours; eyelash effect after 2 months
IR 20 minutes; ER ~6 hours
IR: 30–60 min; XR: 1–2 h to peak effect
IV pulse: hours; PO: hours; intra-articular: days
IV/IM 1-3 minutes; PO 30-60 minutes
IV: 1-3 minutes (SVT termination); PO IR: 30-60 minutes; ER: hours
IV: 3-7 minutes (rate control); PO IR: 30-60 minutes; ER: hours
IV: 5 minutes; PO: 30-60 minutes
IV: 5-20 minutes; PO: 30-60 minutes
IV: minutes; IM benzathine: depot levels last weeks
IV: minutes; oral: weeks to load
Immediate (IV)
Immediate (IV); within minutes (oral antacid)
Immediate intravascular expansion
Inhaled: 5-15 minutes; PO: 30 minutes
Inhaled: bronchial effect 1-2 weeks; nasal: symptom relief 12-24 hours; topical: hours
Inhaled: bronchial effect 1-2 weeks; oral GI effect 1-2 weeks
Intranasal: symptom relief 12-24 hours; inhaled: bronchial effect 1-2 weeks
LDL lowering at 1 week, max by 4 weeks
LDL lowering at 2 weeks, max by 4 weeks; cardiovascular benefit months to years
LDL lowering within 2 weeks
LDL reduction ~50-60% from baseline at 1-2 weeks
Lipid changes 4-8 weeks
Migraine effect after 1-3 months of daily use
Minutes
Modest appetite suppression within weeks; weight loss over months
Mood improvement at 1-3 weeks; full effect 4-6 weeks
Mood: 2–4 weeks. Pain: often within 1–2 weeks.
Mucosal protection within hours; ulcer healing over 2-4 weeks
Natriuresis at 2-3 days; endocrine effects (gynecomastia, antiandrogen action) over weeks
Neuroleptic effect emerges over days to weeks
Neuroleptic effect emerges over days to weeks; activation symptoms (akathisia, insomnia) often within days
Neuropathic pain and fibromyalgia effect emerges over 1-2 weeks
OCD effect over 1-2 weeks initial, with full effect typically 6-12 weeks; among the slowest SSRIs for OCD response
Onset of preventive effect over weeks; some patients respond after first dose
Oral analgesic effect 30-60 minutes; opioid-withdrawal suppression 30 minutes (oral); IV ~10 minutes
Oral peak plasma 1 hour; therapeutic opioid blockade within hours of first dose. IM Vivitrol: peak plasma 2-3 days; therapeutic blockade through the dosing interval.
Oral peak plasma 2.5 hours. Clinical antipsychotic response typically emerges over weeks with continued titration; full response assessment requires 3-6 months at adequate therapeutic levels.
Oral: hours; IV: minutes
PBA episode reduction within 1-2 weeks
PET Aβ reduction over months
PO 1 hour; IV 10 minutes
PO 1–2 h; IM 30–60 min; IV 5–20 min
PO 30-60 minutes; IV minutes
PO 6-12 hours; PR 15-60 minutes
PO: 30-60 minutes; IV: minutes
Pain and migraine prophylaxis effect 1-4 weeks; antidepressant effect 4-6 weeks
Pain relief reported within 15 min in trials
Peak anticoagulant effect 2-4 hours
Peak anticoagulant effect 3-4 hours
Peak plasma at 1-2 hours; clinical effect within 24-72 hours
Peak plasma concentration in 2-4 hours after oral administration. Clinically perceptible wakefulness-promoting effects typically begin within 1-2 hours of dosing.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup>
Prostate volume reduction over 6-12 months
Rapid (within 1 week in trials)
Reticulocyte response at 3-5 days; neurologic recovery weeks to months (and may be incomplete if longstanding)
Reticulocyte response at 7-10 days; hemoglobin rise of ~1 g/dL per 3 weeks
Rheumatologic effect at 4-8 weeks; ectopic resolution over 2-3 weeks
Rheumatologic effect at 6-12 weeks
SC: 5-15 minutes (Fiasp 2.5 minutes earlier on average)
SC: 5-15 minutes; ultra-rapid Lyumjev faster
SL/spray: 1-3 minutes; IV: minutes; patch: 30-60 minutes
SL: 2-5 minutes; PO mononitrate: 30-60 minutes
Seconds
Sedation from first dose; neuroleptic effect emerges over days to weeks
Sedation/dizziness within hours of oral dose; endometrial effects over days
Serum urate falls gradually over days to weeks; acute flare prevention requires colchicine cover during initiation
Significant antidepressant response by week 1 in trials (faster than monoaminergic antidepressants which take 4-6 weeks)
Sleep effect from first dose; analgesic and migraine-prophylaxis effect 1-4 weeks; antidepressant effect 4-6 weeks
Sleep effect within 30-60 minutes; antidepressant effect over 1-2 weeks
Slow, 2–6 h
Slowing of cognitive decline over 18 months (modest effect, ~27% relative slowing)
Smoked 2-5 min; insufflated 5-15 min; oral 30-60 min; IV / IM ~5-15 min
Sublingual analgesic effect 30-60 minutes; MOUD craving suppression within hours; Butrans patch steady-state in 3 days.
Symptom improvement within 1 week; peak effect at 4-6 weeks
Symptom improvement within 1-2 weeks
Symptom improvement within weeks
Symptom relief 1-4 days; full acid suppression after 3-5 days of dosing
Symptom relief within 24-48 hours
Symptom relief within 24-48 hours of starting episodic treatment
Symptom relief within 30 minutes
Symptom relief within 30-60 minutes
Symptom relief within days
Symptom shortening detectable within 24-48 hours of starting (small absolute benefit; ~1 day reduction in symptom duration)
Symptomatic effect within weeks; full response by 12-24 weeks
Symptomatic improvement 2-4 weeks
TSH normalization 4-8 weeks
TSH normalization 4-8 weeks; symptomatic improvement weeks to months
Topical hours; intra-articular days to weeks
Topical hours; oral days
Topical: inflammation, erythema, crusting at 2 weeks; complete response weeks to months after course
Topical: irritation within days; acne improvement 6-12 weeks; oral APL response within days
Triglyceride lowering at 2-4 weeks; max at 8 weeks
Triglyceride lowering at 4-8 weeks
Triglyceride lowering at 4-8 weeks; CV benefit emerges over months
Typical antidepressant 4-6 week onset
Urinary concentration adequate within hours
Vasomotor relief 2-4 weeks; bone density gains over months
Visible lightening at 4-12 weeks
Wake-promoting effect over weeks of titration
Weeks for psychosis/depression; AD agitation benefit emerges over weeks
Weeks for psychosis/mood efficacy
Weeks to raise 25(OH)D into reference range
Within 30 minutes (IR)
Within hours of first administration
Within minutes
~15 min (fastest of the PDE5 inhibitors)
~15–30 min
~20–40 min PO; faster sublingual/intranasal.
~30 minutes (oral)
~30-60 min
Search
duration:
6-8 hours (1)
halflife:
~7-10 hours (variable; longer in renal impairment)'"`UNIQ--ref-00000FB4-QINU`"' (1)
bioavailability:
(Click arrow to add another value)
None
·
100% (IV)
·
~100% from subcutaneous depot
·
~80% (oral)'"`UNIQ--ref-00000027-QINU`"'
·
70–90% (oral)
·
~100% (oral)'"`UNIQ--ref-0000001C-QINU`"'
·
~50% (oral)'"`UNIQ--ref-00000021-QINU`"'
·
~95%
·
'''Saturable''' via the LAT-1 amino-acid transporter, producing nonlinear pharmacokinetics: ~60% at 300 mg single dose, falling to ~35% at 1200 mg single dose'"`UNIQ--ref-0000002A-QINU`"'
·
10-20% (oral; reduced by food, calcium, antacids, PPIs, tea/coffee; enhanced by ascorbate)
·
100% (IV); essentially complete (oral)
·
100% (IV); rapidly neutralized by gastric acid (oral)
·
16-21% capsule, 25% suspension (oral; iron and antacids reduce absorption substantially)'"`UNIQ--ref-000009E5-QINU`"'
·
25 mg: ~29%; 50 mg: ~35%; food reduces absorption'"`UNIQ--ref-00000C4F-QINU`"'
·
30-40% (oral; increases with repeated dosing as gastric pH rises)'"`UNIQ--ref-000000DF-QINU`"'
·
40-45% (oral; not significantly affected by food)'"`UNIQ--ref-0000025C-QINU`"'
·
40-80% (oral); reduced by food, calcium, iron, PPIs, fiber; take fasting with water'"`UNIQ--ref-00000037-QINU`"'
·
42-58% (oral; dose-dependent)'"`UNIQ--ref-00000AEF-QINU`"'
·
50-60% (oral; decreased with food, but food given anyway for GI tolerance)'"`UNIQ--ref-00000019-QINU`"'
·
60-70% PO at low doses; saturable at high doses (parenteral routes preferred above 15-25 mg/week)'"`UNIQ--ref-000007C9-QINU`"'
Other values:
60-80% (oral)
60-80% (oral; not significantly affected by food)'"`UNIQ--ref-00000843-QINU`"'
64-90% (oral; not affected by food)'"`UNIQ--ref-00000079-QINU`"'
65-75% (oral)'"`UNIQ--ref-0000013F-QINU`"'
70-75% (oral)'"`UNIQ--ref-000007ED-QINU`"'
70-80% (oral)'"`UNIQ--ref-000002A4-QINU`"'
75-90% (oral; minimally affected by food)'"`UNIQ--ref-000001A2-QINU`"'
80-90% oral
90% (oral; food delays but does not reduce absorption)'"`UNIQ--ref-000004F3-QINU`"'
<0.1% systemic absorption (PEG 3350 is too large to absorb intact)
<1% (oral; further reduced by food, calcium, iron, antacids; hence the strict fasting/upright dosing rules)'"`UNIQ--ref-000006C4-QINU`"'
<1% oral (extensive first-pass via CYP3A4); ~30% inhaled lung deposition'"`UNIQ--ref-000001DE-QINU`"'
<3% systemic absorption (the basis of the safety and mechanism)'"`UNIQ--ref-00000F5E-QINU`"'
<5% (extensive hepatic first-pass; food enhances absorption of IR, hence the evening-meal dosing)'"`UNIQ--ref-00000808-QINU`"'
<5% (extensive hepatic first-pass; statin pharmacology is hepatocellular, not systemic)'"`UNIQ--ref-0000017B-QINU`"'
<5% systemic absorption (this is the safety basis)'"`UNIQ--ref-00000DC3-QINU`"'
>90% (oral)'"`UNIQ--ref-0000001C-QINU`"'
>90% (oral; food slows absorption and reduces peaks, hence the post-meal dosing rule)'"`UNIQ--ref-000001BD-QINU`"'
>90% (oral; not affected by food or gastric pH — a major practical advantage over itraconazole)'"`UNIQ--ref-00000A48-QINU`"'
>90% (oral; not significantly affected by food)'"`UNIQ--ref-00001120-QINU`"'
Absolute bioavailability not precisely characterized; food modestly increases exposure
Acid-labile; not effective orally (oral form available outside US as penicillin G salts but penicillin V is preferred for oral use)'"`UNIQ--ref-0000141A-QINU`"'
Adequate (food-dependent, must take with fatty meal)
Adequate oral bioavailability
Adequate oral bioavailability with extended-release formulation
Approximately 50-60% (oral; subject to first-pass metabolism); food does not significantly affect absorption.'"`UNIQ--ref-0000004C-QINU`"'
Buprenorphine ~30% SL; naloxone <10% SL (intentional, inactive sublingually, matters only if injected)
Butalbital well-absorbed; aspirin 50-75%; caffeine ~100%'"`UNIQ--ref-000015B8-QINU`"'
Butalbital well-absorbed; caffeine ~100%; acetaminophen 85-98%'"`UNIQ--ref-000015A0-QINU`"'
Carbonate ~30-40% (best with food and acid); citrate ~24% (absorbable without acid; preferred in achlorhydria, PPI use, post-bariatric)
Codeine ~60% (oral); acetaminophen 85-98%'"`UNIQ--ref-00001518-QINU`"'
Essentially zero systemic absorption from oral or topical routes — the topical-action-only profile is the basis of its safety'"`UNIQ--ref-00000D18-QINU`"'
High (oral)
High (oral); not significantly affected by food'"`UNIQ--ref-00000397-QINU`"'
High (oral)'"`UNIQ--ref-00000FB5-QINU`"'
High (oral)'"`UNIQ--ref-00001051-QINU`"'
High (oral)'"`UNIQ--ref-00001165-QINU`"'
High (oral)'"`UNIQ--ref-000012A0-QINU`"'
High (oral; absorption not affected by food)'"`UNIQ--ref-00000825-QINU`"'
High (oral; food enhances)'"`UNIQ--ref-00001039-QINU`"'
High (oral; food prolongs absorption modestly)'"`UNIQ--ref-00000622-QINU`"'
High (oral; not affected by food, but typically given with the morning meal)'"`UNIQ--ref-0000027D-QINU`"'
High (oral; not significantly affected by food)'"`UNIQ--ref-00000B65-QINU`"'
High with fat-containing meal; reduced in malabsorption
Highly formulation-dependent; the goal is colonic delivery with minimal systemic exposure'"`UNIQ--ref-00000BBF-QINU`"'
Highly route-dependent: SL bypasses first-pass; oral has extensive first-pass (used only for chronic ER preparations); transdermal predictable'"`UNIQ--ref-00000C10-QINU`"'
Highly salt-dependent: citrate ~25-30%; oxide ~4% (limited and causes osmotic diarrhea); chloride ~12%
Highly variable due to saturable first-pass metabolism'"`UNIQ--ref-0000002C-QINU`"'
IM/SC ~100%; oral negligible (extensive first-pass and gut metabolism — hence the no-oral route)'"`UNIQ--ref-00000E53-QINU`"'
IV/IM ~100%; inhaled: minimal systemic; oral: negligible (not used orally for systemic infection)'"`UNIQ--ref-000010B4-QINU`"'
Improved with food'"`UNIQ--ref-00000052-QINU`"'
Increased substantially via CYP2D6 inhibition'"`UNIQ--ref-00001584-QINU`"'
Increased with food (varies by formulation; the micronized and nanocrystal forms are less food-dependent)'"`UNIQ--ref-000004AE-QINU`"'
Inhaled lung deposition with minimal systemic absorption (the basis of the favorable safety profile vs systemic antimuscarinics)'"`UNIQ--ref-00000F7C-QINU`"'
Inhaled lung deposition ~20%; systemic absorption from lung ~33%; oral component negligible'"`UNIQ--ref-000009C1-QINU`"'
Intranasal ~40% systemic; ophthalmic minimal'"`UNIQ--ref-000013B7-QINU`"'
Intranasal: <1% systemic; inhaled lung deposition with extensive first-pass clearance'"`UNIQ--ref-00000F9D-QINU`"'
Limited but adequate; take with food
Local (intramuscular)
Local action; minimal systemic effect
Low systemic absorption (enteric coating delivers drug to colon)'"`UNIQ--ref-0000106C-QINU`"'
Mononitrate ~100% (no first-pass; the principal advantage over dinitrate); dinitrate ~20%'"`UNIQ--ref-00001462-QINU`"'
Naltrexone ~5% (oral, extensive first-pass to 6β-naltrexol); bupropion ER ~87%'"`UNIQ--ref-00001569-QINU`"'
Negligible (not absorbed)'"`UNIQ--ref-00000058-QINU`"'
Negligible systemic absorption'"`UNIQ--ref-0000119D-QINU`"'
Not characterized; oral dosing once daily
Not formally characterized for the combination
Not formally characterized in humans.
Not formally established
Not formally established (high SC)
Not formally established; oral once-daily adequate
Not well characterized
Not well characterized'"`UNIQ--ref-00000019-QINU`"'
Olanzapine 60% (oral); fluoxetine high (oral)'"`UNIQ--ref-0000154E-QINU`"'
Oral bioavailability is not precisely established in the label but absorption is rapid and essentially complete. Food delays peak plasma concentration by approximately one hour but does not reduce the extent of absorption.'"`UNIQ--ref-0000006F-QINU`"'
Oral bioavailability of psilocin from administered psilocybin approximately 50%
Oral bioavailability suitable for daily dosing
Oral non-undecanoate has essentially zero bioavailability (hepatic first-pass)
Oral ~1-3% via passive diffusion at high doses (independent of intrinsic factor); IM/SC ~100%
Oral ~5% (extensive first-pass to estrone and conjugates); transdermal bypasses first-pass, giving more physiologic estradiol:estrone ratio'"`UNIQ--ref-000003BB-QINU`"'
Oral ~70%; depot IM provides sustained release over weeks'"`UNIQ--ref-0000101B-QINU`"'
Oral ~90%; depot IM essentially 100% over the dosing interval'"`UNIQ--ref-00000F21-QINU`"'
Oral: very low (extensive first-pass); micronization improves uptake somewhat. Vaginal: high local effect with lower systemic levels (first-uterine-pass concentration)'"`UNIQ--ref-00000727-QINU`"'
Oxycodone 60-87%; aspirin 50-75%'"`UNIQ--ref-000014FB-QINU`"'
Rapid absorption; absolute bioavailability not formally established
Reasonable (not formally established as a percentage)
SC ~47%–65%'"`UNIQ--ref-0000005A-QINU`"'
SC ~55%'"`UNIQ--ref-0000018B-QINU`"'
SC ~65%–75%<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup>
SC ~80%<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup>
SC ~89%<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> · Oral ~0.4–1% (SNAC-enhanced)'"`UNIQ--ref-00000254-QINU`"'
Sandimmune: highly variable (~30%); Neoral microemulsion: ~50%, less variable; '''Sandimmune and Neoral are NOT bioequivalent and not interchangeable''''"`UNIQ--ref-00000A92-QINU`"'
Substantially improved with high-fat meal; take with food'"`UNIQ--ref-000013D2-QINU`"'
Sumatriptan ~15% (oral; substantial first-pass); naproxen ~95%'"`UNIQ--ref-000015D2-QINU`"'
Tablet ~100% relative to oral solution; extensive first-pass metabolism
Topical with limited but measurable systemic absorption'"`UNIQ--ref-00001219-QINU`"'
Topical with measurable systemic absorption (small CA inhibition observed clinically with chronic use)'"`UNIQ--ref-00000B0B-QINU`"'
Topical with minimal systemic absorption'"`UNIQ--ref-000011DA-QINU`"'
Topical with minimal systemic absorption'"`UNIQ--ref-0000123A-QINU`"'
Topical with minimal systemic absorption'"`UNIQ--ref-00001288-QINU`"'
Topical with variable systemic absorption depending on body site, occlusion, and skin integrity; HPA-axis suppression is documented even with brief courses to large areas'"`UNIQ--ref-0000079F-QINU`"'
Topical/intranasal: high local, low systemic; intra-articular: local depot then systemic absorption'"`UNIQ--ref-00000667-QINU`"'
Topical/oral local action with minimal systemic absorption'"`UNIQ--ref-00001399-QINU`"'
Topical: local effect on enamel; systemic supplementation has high oral bioavailability with skeletal accumulation
Topical: minimal systemic absorption (oral systemic 5-FU not used due to poor and variable absorption)'"`UNIQ--ref-000011BF-QINU`"'
Topical: minimal systemic absorption with normal skin; oral: variable, induced metabolism with repeated dosing'"`UNIQ--ref-00000BA4-QINU`"'
Topical: minimal systemic; oral: pH-dependent, requires gastric acid'"`UNIQ--ref-00000889-QINU`"'
Topical: minimal systemic; troche: ~3% systemic'"`UNIQ--ref-00000F46-QINU`"'
Topical; clinically meaningful systemic absorption can produce systemic α2 effects (somnolence, hypotension), especially in children'"`UNIQ--ref-000010D2-QINU`"'
Topical; minimal systemic absorption'"`UNIQ--ref-00000418-QINU`"'
Topical; minimal systemic absorption'"`UNIQ--ref-00000A03-QINU`"'
Topical; minimal systemic absorption'"`UNIQ--ref-00000DA2-QINU`"'
Tramadol ~75% (oral); acetaminophen 85-98%'"`UNIQ--ref-00001531-QINU`"'
Variable (oral; rapidly conjugated to active glucuronide; food does not affect)'"`UNIQ--ref-00000451-QINU`"'
Variable; reduced by food, calcium, iron, PPIs'"`UNIQ--ref-0000001B-QINU`"'
~0.3% (oral; extensive first-pass via CYP3A4 and P-glycoprotein-mediated efflux at the intestinal and blood-brain barriers limit systemic and CNS exposure at therapeutic doses)'"`UNIQ--ref-00000FD3-QINU`"'
~10% inhaled reaches systemic circulation; ~50% PO'"`UNIQ--ref-0000009A-QINU`"'
~100% (oral); highly (~90%) protein-bound, with non-linear binding above therapeutic levels (free fraction matters clinically in hypoalbuminemia)'"`UNIQ--ref-0000097D-QINU`"'
~100% (oral)'"`UNIQ--ref-0000001B-QINU`"'
~100% (oral)'"`UNIQ--ref-00000020-QINU`"'
~100% (oral)'"`UNIQ--ref-00000021-QINU`"'
~100% (oral)'"`UNIQ--ref-00000027-QINU`"'
~100% (oral, but oral use is limited to continuation from parenteral)'"`UNIQ--ref-00000021-QINU`"'
~100% (oral; absorption complete)'"`UNIQ--ref-0000126F-QINU`"'
~100% (oral; food delays absorption, hence pre-meal dosing for IR)'"`UNIQ--ref-000002DA-QINU`"'
~100% (oral; near-complete absorption)'"`UNIQ--ref-00000018-QINU`"'
~100% (oral; not significantly affected by food)'"`UNIQ--ref-00000493-QINU`"'
~100% both components
~100% from subcutaneous depot (by definition of the route)
~12% (extensive metabolizers); ~96% (poor metabolizers)
~14% (extensive hepatic first-pass)'"`UNIQ--ref-0000001C-QINU`"'
~14% (oral; substantial first-pass); ~97% (subcutaneous); ~17% (nasal)'"`UNIQ--ref-00000016-QINU`"'
~15% (extensive hepatic first-pass)
~15% (oral; highly variable due to extensive and variable first-pass metabolism)'"`UNIQ--ref-00000022-QINU`"'
~17% (oral; food slightly reduces absorption)'"`UNIQ--ref-000003D6-QINU`"'
~20% (oral; hydrophilic, minimal CYP metabolism, mostly excreted unchanged in bile)'"`UNIQ--ref-000000FD-QINU`"'
~20% (oral; valacyclovir prodrug raises this to ~55%)'"`UNIQ--ref-00000910-QINU`"'
~20-35% (oral; extensive first-pass via CYP3A4 with R/S enantiomer differences)'"`UNIQ--ref-00000A6C-QINU`"'
~22–25%
~25% (extensive hepatic first-pass)
~25% (high first-pass)
~25% (oral)'"`UNIQ--ref-00000019-QINU`"'
~25% (oral, with extensive first-pass)'"`UNIQ--ref-00000023-QINU`"'
~25% (oral; extensive first-pass)'"`UNIQ--ref-0000001B-QINU`"'
~25% (oral; food does not affect absorption)'"`UNIQ--ref-0000005A-QINU`"'
~25% (oral; food reduces absorption ~40%)'"`UNIQ--ref-000004CE-QINU`"'
~25-35% (extensive first-pass), increased by food which slows absorption and reduces orthostatic risk'"`UNIQ--ref-0000001C-QINU`"'
~25-40% (oral; extensive first-pass)'"`UNIQ--ref-00000021-QINU`"'
~25-50% (oral; substantial first-pass via NAT2 acetylation, phenotype-dependent)'"`UNIQ--ref-00000688-QINU`"'
~26% (oral; prodrug hydrolyzed by intestinal esterases to active olmesartan; not affected by food)'"`UNIQ--ref-0000056D-QINU`"'
~28% (oral; food slows but does not reduce absorption)'"`UNIQ--ref-00000C33-QINU`"'
~30% (high first-pass)
~30% (oral)'"`UNIQ--ref-00000021-QINU`"'
~30% (oral)'"`UNIQ--ref-0000117D-QINU`"'
~30% (sublingual; the primary therapeutic route); ~10-20% (oral swallowed, low due to first-pass); ~50% (buccal Belbuca); transdermal Butrans bypasses first-pass.'"`UNIQ--ref-00000050-QINU`"'
~30-65% (oral; acid-labile, hence enteric-coated formulations; food affects absorption variably)'"`UNIQ--ref-00000D3F-QINU`"'
~33%
~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-QINU`"'
~33% (oral; fruit juices including grapefruit, orange, and apple reduce absorption substantially via OATP1A2 inhibition — distinctive interaction not seen with most other H1s)'"`UNIQ--ref-00000CCD-QINU`"'
~33-55% (IR); reduced by food'"`UNIQ--ref-0000001B-QINU`"'
~35% (oral, extensive first-pass; not used orally for systemic effect); ~100% (IV)'"`UNIQ--ref-00000021-QINU`"'
~36% (oral)'"`UNIQ--ref-00000C93-QINU`"'
~37% (oral, as axetil prodrug; food modestly improves absorption)'"`UNIQ--ref-00000FFA-QINU`"'
~37% (oral; food does not affect)'"`UNIQ--ref-00000A23-QINU`"'
~37% (oral; food reduces absorption modestly)'"`UNIQ--ref-000003FD-QINU`"'
~38% (oral; non-acidic prodrug improves GI tolerability over many other NSAIDs)'"`UNIQ--ref-000011FA-QINU`"'
~4% (extensive first-pass metabolism)'"`UNIQ--ref-0000001E-QINU`"'
~40%
~40% (oral); food and formulation substantially alter the absorption profile'"`UNIQ--ref-0000001E-QINU`"'
~40% (oral; extensive first-pass via CYP3A4)'"`UNIQ--ref-00000643-QINU`"'
~40% (oral; food does not significantly affect)'"`UNIQ--ref-00000EB3-QINU`"'
~40-60% (oral, with significant first-pass)'"`UNIQ--ref-00000027-QINU`"'
~44%
~45% (oral)'"`UNIQ--ref-00000C73-QINU`"'
~45% (oral; substantially higher than sumatriptan's ~14%)'"`UNIQ--ref-00000013-QINU`"'
~45%'"`UNIQ--ref-00000027-QINU`"'
~48% intranasal
~5% intranasal
~5-20% (extensive first-pass), highly variable between individuals'"`UNIQ--ref-00000024-QINU`"'
~5-40% (oral, highly variable due to extensive first-pass metabolism; mean ~5-10% for parent naltrexone with the majority of pharmacologic effect coming from 6-beta-naltrexol). IM Vivitrol bypasses first-pass entirely.'"`UNIQ--ref-00000050-QINU`"'
~50%
~50% (highly variable)
~50% (oral); systemic absorption from ophthalmic application is clinically meaningful via nasolacrimal drainage'"`UNIQ--ref-0000001C-QINU`"'
~50% (oral)'"`UNIQ--ref-00000027-QINU`"'
~50% (oral)'"`UNIQ--ref-000002C5-QINU`"'
~50% (oral; highly variable)'"`UNIQ--ref-00000CB4-QINU`"'
~50% (oral; highly variable, 10-100%, hence the standard 1:2 IV-to-PO conversion)'"`UNIQ--ref-00000223-QINU`"'
~50% (oral; not significantly affected by food)'"`UNIQ--ref-000001FC-QINU`"'
~50% (oral; reduced by buffering and enteric coating but onset clinically similar)'"`UNIQ--ref-00000028-QINU`"'
~50% (oral; substantial first-pass)'"`UNIQ--ref-00000024-QINU`"'
~50% (variable, CYP2D6-dependent for analgesic effect).
~50% IR (extensive first-pass via CYP3A4); ER products release-rate-limited'"`UNIQ--ref-0000074E-QINU`"'
~50-60% (oral; food enhances)
~50-60% (oral; substantial first-pass metabolism)'"`UNIQ--ref-0000002A-QINU`"'
~53% (oral)'"`UNIQ--ref-00000024-QINU`"'
~55% (oral)'"`UNIQ--ref-00000016-QINU`"'
~55% bioavailability of acyclovir after valacyclovir oral (vs ~20% from oral acyclovir directly)'"`UNIQ--ref-000005D7-QINU`"'
~58% (extended-release); ~80% (immediate-release)'"`UNIQ--ref-00000021-QINU`"'
~6% IR oral (substantial first-pass to active N-desethyl metabolite, which contributes most of the antimuscarinic adverse effects); transdermal bypasses first-pass and is better tolerated'"`UNIQ--ref-000006E2-QINU`"'
~6-13% inhaled lung deposition; ~10% oral (Entocort EC; extensive first-pass via CYP3A4 — this is the basis of the favorable hepatic-targeted local-effect profile in IBD)'"`UNIQ--ref-000009A6-QINU`"'
~60%
~60% (oral); ~100% (IM)'"`UNIQ--ref-00000027-QINU`"'
~60% (oral)'"`UNIQ--ref-00000379-QINU`"'
~60% (oral)'"`UNIQ--ref-00000D5A-QINU`"'
~60% (oral; food does not affect absorption)'"`UNIQ--ref-00000B85-QINU`"'
~60% (oral; phenoxymethyl modification makes it acid-stable, unlike penicillin G which is destroyed by gastric acid)'"`UNIQ--ref-00000E77-QINU`"'
~60% (oral; substantially increased with high-fat meal)'"`UNIQ--ref-00001093-QINU`"'
~60% from subcutaneous depot (reduced by reversible albumin binding via the myristic acid side chain that also extends duration)'"`UNIQ--ref-00001375-QINU`"'
~60-87% (oral; high and more consistent than codeine or hydrocodone, making efficacy less CYP2D6-genotype-dependent)'"`UNIQ--ref-0000001E-QINU`"'
~60-87% oxycodone (high and predictable, less CYP-genotype-dependent than codeine or hydrocodone); 85-98% acetaminophen'"`UNIQ--ref-000014E3-QINU`"'
~60–70% (oral)
~62%
~63% (oral)'"`UNIQ--ref-00000532-QINU`"'
~63% (oral; extensive first-pass)'"`UNIQ--ref-00000015-QINU`"'
~64% (oral)'"`UNIQ--ref-00000016-QINU`"'
~64% (oral; not significantly affected by food)'"`UNIQ--ref-0000015F-QINU`"'
~64% from SC depot'"`UNIQ--ref-00001104-QINU`"'
~64-90% (oral; increases at higher doses and with multi-day dosing)'"`UNIQ--ref-000008E9-QINU`"'
~65% (oral)'"`UNIQ--ref-00000022-QINU`"'
~65% (oral)'"`UNIQ--ref-00000784-QINU`"'
~65% (oral)'"`UNIQ--ref-00000AB1-QINU`"'
~65% (oral)'"`UNIQ--ref-000013F6-QINU`"'
~67% (oral)'"`UNIQ--ref-00000B26-QINU`"'
~70% (oral)'"`UNIQ--ref-0000001B-QINU`"'
~70% (oral)'"`UNIQ--ref-00000022-QINU`"'
~70% (oral)'"`UNIQ--ref-000008C5-QINU`"'
~70% (oral; bioavailability and absorption are improved with food)'"`UNIQ--ref-00000355-QINU`"'
~70% (oral; reduced by divalent cations — antacids, iron, calcium, dairy)'"`UNIQ--ref-00000939-QINU`"'
~70-85% (oral)'"`UNIQ--ref-00000027-QINU`"'
~70-85% (oral, high relative to other opioids)
~70-90% at typical doses; saturable at high doses (>500 mg)
~72% (with food); much lower fasting (~36%)
~72% from SC depot'"`UNIQ--ref-00001480-QINU`"'
~72% oral; ~85% smoked'"`UNIQ--ref-00000066-QINU`"'
~75%
~75% (IR, rises with multi-dose administration due to saturable first-pass)'"`UNIQ--ref-00000025-QINU`"'
~75% (oral, as the active carboxylate after hepatic esterase activation)'"`UNIQ--ref-00000E95-QINU`"'
~75% (oral; absorption improved with fat-containing meal)
~75% (oral; fat-soluble, absorption requires intact biliary/lipid digestion)'"`UNIQ--ref-00000331-QINU`"'
~75-85% (oral); ~60% (transdermal at steady state)'"`UNIQ--ref-00000027-QINU`"'
~75–90% (oral)
~77% (oral; not affected by food or antacids)'"`UNIQ--ref-0000011E-QINU`"'
~78% (oral; high-fat meal modestly reduces but is not clinically significant)'"`UNIQ--ref-00000553-QINU`"'
~80% (oral)'"`UNIQ--ref-0000001B-QINU`"'
~80% (oral)'"`UNIQ--ref-0000001E-QINU`"'
~80% (oral)'"`UNIQ--ref-00000029-QINU`"'
~80% (oral)'"`UNIQ--ref-00000310-QINU`"'
~80% (oral)'"`UNIQ--ref-00000BEC-QINU`"'
~80% (oral)'"`UNIQ--ref-00000E2C-QINU`"'
~80% (oral; predictable absorption — a substantive practical advantage over furosemide whose oral absorption is 10-100% variable)'"`UNIQ--ref-00000B47-QINU`"'
~80% (oral; reduced by significant first-pass)'"`UNIQ--ref-00000EFA-QINU`"'
~80-100% (oral)'"`UNIQ--ref-00000027-QINU`"'
~80-100% with food at 15-20 mg doses (10 mg dose: ~80% without food); '''must be taken with food''' at therapeutic doses'"`UNIQ--ref-00000514-QINU`"'
~80-95% (oral; more reliable than furosemide, comparable to torsemide)'"`UNIQ--ref-00000DE4-QINU`"'
~80-99% (oral)'"`UNIQ--ref-00000868-QINU`"'
~82%
~82% SC
~85-90% (oral; not significantly affected by food)'"`UNIQ--ref-00000955-QINU`"'
~85-98% (oral)'"`UNIQ--ref-00000023-QINU`"'
~87% (oral)'"`UNIQ--ref-00000026-QINU`"'
~87% (oral)'"`UNIQ--ref-00000766-QINU`"'
~89% (oral)'"`UNIQ--ref-00000021-QINU`"'
~90% (low first-pass)
~90% (oral)'"`UNIQ--ref-00000018-QINU`"'
~90% (oral)'"`UNIQ--ref-00000027-QINU`"'
~90% (oral)'"`UNIQ--ref-0000002A-QINU`"'
~90% (oral)'"`UNIQ--ref-00000DFF-QINU`"'
~90% (oral)'"`UNIQ--ref-00001140-QINU`"'
~90% (oral)'"`UNIQ--ref-00001443-QINU`"'
~90% (oral, low first-pass)'"`UNIQ--ref-0000001C-QINU`"'
~90% (oral; food increases absorption)'"`UNIQ--ref-000008A4-QINU`"'
~90% (oral; not affected by food but reduced by divalent cations)'"`UNIQ--ref-00000D83-QINU`"'
~93% (oral); ~90% (rectal)'"`UNIQ--ref-0000002B-QINU`"'
~93% (oral)'"`UNIQ--ref-00000ED4-QINU`"'
~95% (oral)'"`UNIQ--ref-0000001B-QINU`"'
~95% (oral)'"`UNIQ--ref-0000001F-QINU`"'
~95% (oral)'"`UNIQ--ref-0000002A-QINU`"'
~95% (oral)'"`UNIQ--ref-000014C4-QINU`"'
~95% (oral; reduced by dairy, antacids, iron via divalent-cation chelation, though less than for tetracycline itself)'"`UNIQ--ref-0000047E-QINU`"'
~96% (oral)'"`UNIQ--ref-00000AD2-QINU`"'
~96% after red blood cell hydrolytic cleavage releases dextroamphetamine'"`UNIQ--ref-00000018-QINU`"'
~98% (oral)'"`UNIQ--ref-00000026-QINU`"'
~99% (caffeine)
~99% (oral)'"`UNIQ--ref-0000002A-QINU`"'
~99% (oral; matched 1:1 IV-to-PO conversion)'"`UNIQ--ref-00000CF6-QINU`"'
≥90% (linear pharmacokinetics, distinguishing it favorably from gabapentin's saturable LAT-1 absorption)'"`UNIQ--ref-00000027-QINU`"'
Search
pregnancy:
Limited data; not first-line in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1)
legal:
OTC (lower doses) and [[USLegal:Prescription only|Rx-only]] (higher doses) in US (1)
Error in "where" parameter: the string "--" cannot be used within #cargo_query.
There are no results for this report.
Search
Search
Drilldown: Medicines
Add topic
& onset:
Symptom relief within 30 minutes 
generic:
mechanism: (Click arrow to add another value)