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; mechanism incompletely understood 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; NMDA antagonist 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) Multi-receptor antagonist; low D2 affinity 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 agonist; kappa antagonist 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 TBD 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-00000040-QINU`"' '"`UNIQ--vote-00000041-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-00000017-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-00000018-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-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-00000032-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-00000033-QINU`"'. '"`UNIQ--vote-00000037-QINU`"' Hypertonic 3% is the standard urgent treatment of severely symptomatic hyponatremia'"`UNIQ--ref-00000038-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
:
Anticonvulsant 
generic:
classes: (Click arrow to add another value)