Drilldown: Medicines

Bromazolam (1) · Cyanocobalamin (vitamin B12) (1) · Dexamethasone (1) · Melatonin (N-acetyl-5-methoxytryptamine) (1) · Methylprednisolone (1) · Nitroglycerin (glyceryl trinitrate, GTN) (1) · Triamcinolone (acetonide and other esters) (1) · Zolpidem (tartrate) (1)

(none, never marketed) (1) · Ambien (IR), Ambien CR (biphasic-release), Edluar (sublingual), Intermezzo (low-dose sublingual for middle-of-night awakening), Zolpimist (oral spray) (1) · Decadron (historical), Dexpak (taper pack), Hemady, Ozurdex (intravitreal) (1) · Kenalog (injectable), Nasacort (intranasal), Aristocort (topical), Trianex (1) · Many OTC and Rx; Nascobal (intranasal); generic injection (1) · Medrol (oral), Solu-Medrol (IV/IM), Depo-Medrol (depot injection) (1) · Multiple OTC dietary supplement formulations (1) · Nitrostat, Nitrolingual, NitroMist, Nitro-Bid, Nitro-Dur, Minitran, Rectiv (1)

Designer benzodiazepine (1) · high-potency)]] (1) · Research material (1) · Sedative-Hypnotic (1) · Triazolobenzodiazepine (1) · [[:Category:Antianginals|Antianginal]] (1) · [[:Category:B-vitamins|B-vitamin]] (1) · [[:Category:Chronobiotics|Chronobiotic (circadian phase regulator)]] (1) · [[:Category:Corticosteroids|Corticosteroid]] (3) · [[:Category:Glucocorticoids|Glucocorticoid (intermediate-acting)]] (2) · [[:Category:Glucocorticoids|Glucocorticoid (long-acting (1) · [[:Category:Hematinics|Hematinic]] (1) · [[:Category:Immunosuppressants|Immunosuppressant]] (2) · [[:Category:Melatonin receptor agonists|Melatonin receptor agonist]] (1) · [[:Category:Nitrates|Organic nitrate]] (1) · [[:Category:Non-benzodiazepine hypnotics|Non-benzodiazepine hypnotic]] (1) · [[:Category:Schedule IV controlled substances|Schedule IV controlled substance]] (1) · [[:Category:Sleep aids|Sleep aid]] (2) · [[:Category:Vasodilators|Vasodilator]] (1) · [[:Category:Vitamins|Vitamin]] (1)

None (6) · Positive allosteric modulator of the GABA_A receptor at the benzodiazepine binding site; increases frequency of Cl⁻ channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1) · '"`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`"'. (1)

No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"' (1) · '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"' (1) · '"`UNIQ--vote-00000607-QINU`"', '"`UNIQ--vote-00000608-QINU`"', '"`UNIQ--vote-00000609-QINU`"', '"`UNIQ--vote-0000060A-QINU`"' (1) · '"`UNIQ--vote-00000661-QINU`"', '"`UNIQ--vote-00000662-QINU`"', '"`UNIQ--vote-00000663-QINU`"', '"`UNIQ--vote-00000664-QINU`"', '"`UNIQ--vote-00000665-QINU`"' (1) · '"`UNIQ--vote-00000862-QINU`"', '"`UNIQ--vote-00000863-QINU`"', '"`UNIQ--vote-00000864-QINU`"', '"`UNIQ--vote-00000865-QINU`"', '"`UNIQ--vote-00000866-QINU`"' (1) · '"`UNIQ--vote-00000C0A-QINU`"', '"`UNIQ--vote-00000C0B-QINU`"', '"`UNIQ--vote-00000C0C-QINU`"', '"`UNIQ--vote-00000C0D-QINU`"', '"`UNIQ--vote-00000C0E-QINU`"' (1) · '"`UNIQ--vote-00000E23-QINU`"', '"`UNIQ--vote-00000E24-QINU`"', '"`UNIQ--vote-00000E25-QINU`"', '"`UNIQ--vote-00000E26-QINU`"', '"`UNIQ--vote-00000E27-QINU`"', '"`UNIQ--vote-00000E28-QINU`"', '"`UNIQ--vote-00000E29-QINU`"', '"`UNIQ--vote-00000E2A-QINU`"' (1)

'''5 mg PO at bedtime for women, 5-10 mg for men''' (per FDA's 2013 sex-specific dose reduction for women due to slower clearance). Ambien CR 6.25 mg women / 6.25-12.5 mg men. Intermezzo SL 1.75 mg women / 3.5 mg men (1) · 0.5-3 mg PO 30-60 minutes before bedtime. Some patients respond to micro-doses (0.3 mg) without additional benefit at higher doses. For circadian phase shifting, timing relative to dim-light melatonin onset matters more than absolute dose (1) · Indication-specific: 0.5-9 mg PO/IV daily for inflammation; 4 mg IV q6h for cerebral edema; 40 mg PO once weekly in MM; 6 mg PO/IV daily ×10 days for severe COVID-19; 0.6 mg/kg PO single dose for croup (max 16 mg) (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · PO Medrol Dosepak (5-day taper from 24 mg to 4 mg) is the prototypic short-course outpatient regimen; IV pulse 1 g daily for 3-5 days for MS relapse; intra-articular 4-80 mg per joint q1-5 weeks (1) · Replacement: 1000 mcg IM daily for 1 week, then weekly for 4 weeks, then monthly; or 1000-2000 mcg PO daily (effective even in pernicious anemia via passive diffusion); intranasal 500 mcg weekly (1) · SL 0.3-0.6 mg every 5 minutes up to 3 doses for acute angina (call EMS if not resolved after the third); IV infusion 5-10 mcg/min titrated; transdermal patch 0.2-0.4 mg/hr for 12-14 hours daily (nitrate-free interval prevents tolerance) (1) · Topical 0.025-0.5% cream/ointment BID; intra-articular 5-40 mg per joint q3-6 months; intranasal Nasacort 110 mcg/spray, 2 sprays/nostril daily; oral paste 0.1% to lesion 2-3×/d (1)

0.5, 0.75, 1, 1.5, 2, 4, 6 mg tablets; oral solution; 4, 10, 20, 100 mg/mL IV; intravitreal implant (Ozurdex) (1) · 100, 250, 500, 1000, 5000 mcg tablets (OTC and Rx); 1000 mcg/mL injection; intranasal spray; sublingual (1) · 2, 4, 8, 16, 32 mg oral tablets; 40, 125, 500, 1000 mg IV vials; Depo-Medrol 20, 40, 80 mg/mL IM depot (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · IR tablets 5, 10 mg; CR tablets 6.25, 12.5 mg; SL tablets 1.75, 3.5, 5, 10 mg; oral spray (1) · OTC tablets, sublingual tablets, gummies, liquid, extended-release tablets and capsules; common strengths 0.5, 1, 3, 5, 10 mg (1) · SL 0.3, 0.4, 0.6 mg tablets; lingual spray 0.4 mg/spray; ER 2.5-9 mg capsules; transdermal patch 0.1-0.8 mg/hr; 2% ointment; 0.4% rectal ointment; 5 mg/mL IV (1) · Topical creams, ointments, lotions, dental paste (0.025-0.5%); Kenalog 10 mg/mL, 40 mg/mL injection; Nasacort 55 mcg/spray intranasal; oral inhaler discontinued in US (1)

10 mg/day (IR); 12.5 mg/day (CR) (1) · Indication-specific (3) · Indication-specific; titrated to effect (1) · N/A (never approved) (1) · No strict ceiling; water-soluble vitamin, low toxicity (1) · Not formally established (dietary supplement); doses above ~3-5 mg show no additional efficacy but increase next-day sedation risk (1)

None · Oral · IV · topical · IM · intranasal · rectal · Subcutaneous · Topical ophthalmic · ophthalmic · intramuscular · intravenous · transdermal · vaginal · Subcutaneous (abdomen · sublingual · thigh · inhaled · SC · intra-articular

Other values:

Search

15-30 minutes (1) · 30-60 minutes (immediate-release oral) (1) · Hours (1) · IV pulse: hours; PO: hours; intra-articular: days (1) · Reticulocyte response at 3-5 days; neurologic recovery weeks to months (and may be incomplete if longstanding) (1) · SL/spray: 1-3 minutes; IV: minutes; patch: 30-60 minutes (1) · Topical hours; intra-articular days to weeks (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

3-4 hours (1) · 6-8 hours (IR); 8 hours (CR via biphasic release) (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Biologic 12-36 hours (intermediate-acting); Depo-Medrol depot weeks (1) · Biologic 36-72 hours (long-acting) (1) · Intra-articular 3-6 months (depot effect of acetonide microcrystals) (1) · N/A (replacement) (1) · SL: 30 minutes; patch: 12-14 hours; IV continuous (1)

1-3 minutes (very short)'"`UNIQ--ref-00000C0F-QINU`"' (1) · 30-50 minutes (short)'"`UNIQ--ref-00000021-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · Plasma 2-3 hours; biologic ~18-36 hours'"`UNIQ--ref-00000867-QINU`"' (1) · Plasma ~3-4.5 hours; biologic ~36-72 hours'"`UNIQ--ref-00000E2B-QINU`"' (1) · Plasma ~3-5 hours; biologic effect substantially longer (~12-36 hours for intermediate-acting glucocorticoids)'"`UNIQ--ref-00000666-QINU`"' (1) · ~2.5 hours'"`UNIQ--ref-0000001A-QINU`"' (1) · ~6 days (plasma); hepatic stores last 3-5 years (1)

Highly route-dependent: SL bypasses first-pass; oral has extensive first-pass (used only for chronic ER preparations); transdermal predictable'"`UNIQ--ref-00000C10-QINU`"' (1) · Not formally characterized in humans. (1) · Oral ~1-3% via passive diffusion at high doses (independent of intrinsic factor); IM/SC ~100% (1) · Topical/intranasal: high local, low systemic; intra-articular: local depot then systemic absorption'"`UNIQ--ref-00000667-QINU`"' (1) · ~15% (oral; highly variable due to extensive and variable first-pass metabolism)'"`UNIQ--ref-00000022-QINU`"' (1) · ~70% (oral)'"`UNIQ--ref-0000001B-QINU`"' (1) · ~80% (oral)'"`UNIQ--ref-00000E2C-QINU`"' (1) · ~80-99% (oral)'"`UNIQ--ref-00000868-QINU`"' (1)

Avoid. Benzodiazepines are associated with neonatal sedation, floppy-infant syndrome, and withdrawal; teratogenic signal weak but non-zero. Designer benzo with no safety data, assume worst-case. (1) · Limited human data; case reports of neonatal sedation with late-pregnancy exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; endogenous hormone, but supplemental pharmacological doses are not well characterized in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Routinely supplemented in vegan pregnancies and pernicious anemia.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Topical/intranasal generally low-risk; intra-articular and high-dose injection: weigh risk individually.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Use when benefits outweigh; small association with oral clefts in first trimester debated.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Used in antenatal lung maturation (24-34 weeks gestation; 6 mg IM q12h × 4 doses); broader use weighs benefits against fetal HPA suppression.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Used in obstetric emergencies (uterine relaxation, severe hypertension) when needed; otherwise limited routine use.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

None (1) · OTC (low/mid-dose oral) and [[USLegal:Prescription only|Rx-only]] (injection, intranasal) in US (1) · OTC (lowest-strength topicals) and [[USLegal:Prescription only|Rx-only]] (higher strengths, injectable) in US (1) · [[USLegal:Over-the-counter|OTC]] dietary supplement in the US ('''not FDA-regulated as a medicine'''; multiple studies show OTC products contain 50-470% of labeled melatonin content); [[USLegal:Prescription only|Rx-only]] in the EU and UK (1) · [[USLegal:Prescription only|Rx-only]] in US (3) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the FDA '''Boxed Warning''' for '''complex sleep behaviors''' (sleep-driving, sleep-walking, sleep-eating, other parasomnias) added in 2019'"`UNIQ--ref-0000001C-QINU`"' (1)