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Choose a table:
Medicines (732)
Medicines
> onset
:
Mood: 2–4 weeks. Pain: often within 1–2 weeks.
or
Postprandial glucose effect within days; HbA1c by 12 weeks
&
bioavailability:
~87% (oral)'"`UNIQ--ref-00000766-QINU`"'
Use the filters below to narrow your results.
generic:
Sitagliptin (1)
brand:
Januvia; with metformin Janumet/Janumet XR (1)
classes:
[[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (1)
·
[[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (1)
·
[[:Category:Incretin_modulators|Incretin pathway modulator]] (1)
mechanism:
'"`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`"'. (1)
uses:
'"`UNIQ--vote-00000764-QINU`"' (1)
starting dose:
100 mg PO once daily (50 mg if CrCl 30-44; 25 mg if <30 or dialysis) (1)
preparations:
25, 50, 100 mg tablets; combination tablets with metformin (1)
fda max:
100 mg/d (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:
24 hours (1)
halflife:
~12.4 hours'"`UNIQ--ref-00000765-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`"'
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pregnancy:
Limited data; switch to insulin where feasible.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1)
legal:
[[USLegal:Prescription only|Rx-only]] in US (1)
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:
Mood: 2–4 weeks. Pain: often within 1–2 weeks. 
generic:
onset: (Click arrow to add another value)