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Medicines (732)

Medicines > classes

: Analgesic

or Sedative-Hypnotic

or [[:Category:Statins|Statin]]

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Codeine (2)

None (14)

None (5) · Extremely potent GABAA positive allosteric modulator (1) · GABAA positive allosteric modulator (15) · GABAA positive allosteric modulator (non-benzodiazepine) (3) · GABAA positive allosteric modulator; very long half-life (1) · GABAA potentiator (1) · GABAA potentiator and direct activator (2) · GABAB agonist; GHB receptor agonist (1) · Kappa agonist; mu antagonist (1) · Kappa agonist; mu partial agonist (1) · Kappa agonist; mu partial agonist/antagonist (1) · Melatonin receptor agonist (2) · Mu-opioid agonist; norepinephrine reuptake inhibitor (1) · Mu-opioid receptor agonist (4) · Mu-opioid receptor agonist; NMDA antagonist (1) · Mu-opioid receptor agonist; prodrug (metabolized to morphine) (1) · Mu-opioid receptor agonist; sodium channel blocker (1) · Mu/kappa/delta agonist; NMDA antagonist (1) · Partial mu-opioid agonist; kappa antagonist (1) · Phosphodiesterase inhibitor; calcium channel blocker (1) · Positive allosteric modulator of the GABAA receptor at the benzodiazepine binding site; increases frequency of Cl− channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1) · Potent mu-opioid receptor agonist (3) · Prodrug; converted to [[Morphine|morphine]] by [[Enzyme:CYP2D6|CYP2D6]] for analgesic action. (1) · Selective GABAA agonist (extrasynaptic delta subunit) (1) · '"`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`"'. (1) · '"`UNIQ--vote-000003D1-QINU`"' SLCO1B1 polymorphism affects exposure but is most clinically actionable for simvastatin'"`UNIQ--ref-000003D2-QINU`"'. (1)

None (46) · Mild to moderate pain; cough suppression (low-dose). (1) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"' (1) · '"`UNIQ--vote-000000F9-QINU`"', '"`UNIQ--vote-000000FA-QINU`"', '"`UNIQ--vote-000000FB-QINU`"' (1) · '"`UNIQ--vote-00000178-QINU`"', '"`UNIQ--vote-00000179-QINU`"' (1) · '"`UNIQ--vote-000003D3-QINU`"', '"`UNIQ--vote-000003D4-QINU`"' (1) · '"`UNIQ--vote-00000805-QINU`"', '"`UNIQ--vote-00000806-QINU`"' (1)

None (46) · 10-20 mg PO once daily (1) · 10-20 mg PO once daily (5 mg in Asian ancestry, elderly, hypothyroidism, or strong CYP/SLCO1B1 interactions) (1) · 10-20 mg PO once daily in the evening (40 mg starting allowed for high CV risk) (1) · 20 mg PO once daily with the evening meal; titrate to 40-80 mg/d (1) · 40 mg PO once daily (10-20 mg in elderly, hepatic impairment, or strong drug interactions) (1) · Adult: 15–60 mg every 4 hours as needed. (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

None (46) · 10 mg, 20 mg, 40 mg, 80 mg tablets (2) · 10, 20, 40 mg tablets; 20, 40, 60 mg ER tablets (1) · 5, 10, 20, 40 mg tablets (1) · 5, 10, 20, 40, 80 mg tablets; 4 mg/mL oral suspension (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) · Tablet (15, 30, 60 mg); oral solution; combination products (with [[Acetaminophen|acetaminophen]] or ibuprofen). (1)

None (46) · 360 mg/day (1) · 40 mg/d (rarely needed; 40 mg restricted to patients not at goal on 20 mg) (1) · 40 mg/d standard; 80 mg/d restricted to patients tolerating 80 mg for ≥12 months without myopathy (post-SEARCH 2011 FDA restriction) (1) · 80 mg/d (2) · 80 mg/d (40 mg/d if combined with diltiazem, verapamil, danazol; lower limits with various interactions) (1) · N/A (never approved) (1)

None (46) · intranasal; rectal and IV reported. (1) · Oral (6) · PO (only formulation marketed in the US). (1) · sublingual (1)

None (46) · 30–60 min (PO) (1) · LDL lowering at 1 week, max by 4 weeks (1) · LDL lowering at 2 weeks, max by 4 weeks (3) · LDL lowering at 2 weeks, max by 4 weeks; cardiovascular benefit months to years (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (46) · 24 hours (3) · 24 hours (evening dosing aligns with overnight HMG-CoA reductase peak) (1) · 24-48 hours per dose (1) · 4–6 hours (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1)

None (46) · 14 hours (parent); 20-30 hours including active ortho- and para-hydroxylated metabolites'"`UNIQ--ref-0000001B-QINU`"' (1) · 2.5–3 hours (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~19 hours'"`UNIQ--ref-000000FC-QINU`"' (1) · ~2 hours (parent and active β-hydroxy acid metabolite); pharmacodynamic effect lasts 24 hours via target turnover'"`UNIQ--ref-0000017A-QINU`"' (1) · ~2-3 hours (parent); pharmacodynamic effect 24 hours via target turnover'"`UNIQ--ref-000003D5-QINU`"' (1) · ~2-4 hours (parent and active β-hydroxy acid metabolite); pharmacodynamic effect 24 hours via target turnover'"`UNIQ--ref-00000807-QINU`"' (1)

None (46) · <5% (extensive hepatic first-pass; food enhances absorption of IR, hence the evening-meal dosing)'"`UNIQ--ref-00000808-QINU`"' (1) · <5% (extensive hepatic first-pass; statin pharmacology is hepatocellular, not systemic)'"`UNIQ--ref-0000017B-QINU`"' (1) · Not formally characterized in humans. (1) · ~14% (extensive hepatic first-pass)'"`UNIQ--ref-0000001C-QINU`"' (1) · ~17% (oral; food slightly reduces absorption)'"`UNIQ--ref-000003D6-QINU`"' (1) · ~20% (oral; hydrophilic, minimal CYP metabolism, mostly excreted unchanged in bile)'"`UNIQ--ref-000000FD-QINU`"' (1) · ~50% (variable, CYP2D6-dependent for analgesic effect). (1)

None (46) · 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) · Avoid; risk of neonatal opioid withdrawal with chronic use; UM-mother breastfeeding contraindicated. (1) · Previously Category X; FDA removed the blanket statin contraindication in pregnancy in 2021. Use individualized.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Previously Category X; FDA removed the blanket statin contraindication in pregnancy in 2021. Use individualized; lactation generally avoided.[[[Pharmacopedia:Citation needed|citation needed]]] (1) · Previously Category X; FDA removed the blanket statin contraindication in pregnancy in 2021.[[[Pharmacopedia:Citation needed|citation needed]]] (3)

None (47) · US Schedule II (single-entity); Schedule III–V (combination products by content). (1) · [[USLegal:Prescription only|Rx-only]] in US (5)

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