Drilldown/Medicines
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generic:
brand:
None (35) ·
(none, never marketed) (1) ·
Calan, Calan SR, Verelan, Verelan PM, Isoptin SR (1) ·
Cardizem, Tiazac, Cartia XT, Dilacor XR, Taztia XT, Matzim LA (1) ·
Dalmane (1) ·
Doral (1) ·
Doriden (1) ·
Halcion (1) ·
Hetlioz (1) ·
Imdur (mononitrate ER), Isordil (dinitrate); generics; with hydralazine as BiDil for HFrEF in self-identified Black patients (1) ·
Imovane (1) ·
Lunesta (1) ·
Mogadon (1) ·
Nembutal (1) ·
Nitrostat, Nitrolingual, NitroMist, Nitro-Bid, Nitro-Dur, Minitran, Rectiv (1) ·
Norvasc, Katerzia (1) ·
Placidyl (1) ·
Procardia, Procardia XL, Adalat CC, Afeditab CR (1) ·
ProSom (1) ·
Quaalude (1) ·
Restoril (1) ·
Rohypnol (1) ·
Rozerem (1) ·
Seconal (1) ·
Sonata (1) ·
THIP (1) ·
Versed (1) ·
Xyrem (1)
classes: (Click arrow to add another value)
mechanism:
None (6) ·
5-HT2A agonist (15) ·
5-HT2A agonist; 5-HT3 antagonist (1) ·
5-HT2A agonist; minor psilocybin mushroom alkaloid (1) ·
5-HT2A agonist; primarily auditory effects (1) ·
5-HT2A agonist; sigma-1 agonist (1) ·
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) ·
Melatonin receptor agonist (2) ·
Monoamine releasing agent; 5-HT2A agonist; MAO inhibitor (1) ·
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. (1) ·
Potent 5-HT2A agonist; sigma-1 agonist (1) ·
Prodrug of 4-HO-DET; 5-HT2A agonist (1) ·
Prodrug of 4-HO-DiPT; 5-HT2A agonist (1) ·
Prodrug of 4-HO-MET; 5-HT2A agonist (1) ·
Prodrug of 4-HO-MiPT; 5-HT2A agonist (1) ·
Prodrug of psilocin; 5-HT2A agonist (1) ·
Selective GABAA agonist (extrasynaptic delta subunit) (1) ·
'"`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`"'. (1) ·
'"`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`"'. (1)
uses:
None (55) ·
No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) ·
'"`UNIQ--vote-00000075-QINU`"', '"`UNIQ--vote-00000076-QINU`"', '"`UNIQ--vote-00000077-QINU`"' (1) ·
'"`UNIQ--vote-0000063E-QINU`"', '"`UNIQ--vote-0000063F-QINU`"', '"`UNIQ--vote-00000640-QINU`"', '"`UNIQ--vote-00000641-QINU`"' (1) ·
'"`UNIQ--vote-00000747-QINU`"', '"`UNIQ--vote-00000748-QINU`"', '"`UNIQ--vote-00000749-QINU`"', '"`UNIQ--vote-0000074A-QINU`"', '"`UNIQ--vote-0000074B-QINU`"', '"`UNIQ--vote-0000074C-QINU`"' (1) ·
'"`UNIQ--vote-00000A66-QINU`"', '"`UNIQ--vote-00000A67-QINU`"', '"`UNIQ--vote-00000A68-QINU`"', '"`UNIQ--vote-00000A69-QINU`"', '"`UNIQ--vote-00000A6A-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-0000145E-QINU`"', '"`UNIQ--vote-0000145F-QINU`"', '"`UNIQ--vote-00001460-QINU`"' (1)
starting dose:
None (55) ·
2.5-5 mg PO once daily; titrate to 10 mg/d (1) ·
ER 180-240 mg PO once daily; IR 30 mg PO QID; IV 0.25 mg/kg over 2 min for acute rate control, then 5-15 mg/h infusion (1) ·
ER 30-60 mg PO once daily; immediate-release 10 mg PO TID (now rarely used for hypertension due to reflex tachycardia) (1) ·
IR 80-120 mg PO TID; ER 180-240 mg PO daily; IV 2.5-5 mg over 2 min for SVT termination (under monitoring); cluster prophylaxis up to 480-960 mg/d in divided doses (1) ·
Isosorbide mononitrate ER: 30-60 mg PO once daily in the morning, titrate to 120-240 mg/d; isosorbide dinitrate IR: 5-20 mg PO TID with a 12-14 hour nitrate-free interval to prevent tolerance (1) ·
No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (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)
preparations:
None (55) ·
10, 20 mg IR capsules; 30, 60, 90 mg ER tablets (1) ·
2.5, 5, 10 mg tablets; 1 mg/mL oral suspension (1) ·
Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1) ·
IR 30, 60, 90, 120 mg tablets; multiple ER capsules and tablets 60-420 mg; IV 5 mg/mL (1) ·
IR 40, 80, 120 mg tablets; SR/ER 100-360 mg; IV 2.5 mg/mL (1) ·
Mononitrate 10, 20 mg IR; 30, 60, 120 mg ER; dinitrate 5, 10, 20, 30, 40 mg IR and ER (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)
fda max:
None (55) ·
10 mg/d (1) ·
120 mg/d (ER); IR not for chronic hypertension (1) ·
240 mg/d (mononitrate ER); 160 mg/d (dinitrate) (1) ·
Indication-specific; titrated to effect (1) ·
N/A (never approved) (1) ·
~480 mg/d (oral) for cardiovascular indications; higher off-label for cluster (1) ·
~480 mg/d (oral); IV per protocol (1)
routes:
None (55) ·
intranasal; rectal and IV reported. (1) ·
IV (3) ·
lingual spray (1) ·
MI reports) (1) ·
multiple ER formulations) (1) ·
Oral (3) ·
Oral (IR (1) ·
Oral (IR and multiple ER) (1) ·
oral ER (1) ·
Oral; sublingual IR is discouraged (uncontrolled BP drops (1) ·
rectal (1) ·
sublingual (2) ·
sublingual (dinitrate) (1) ·
topical (1) ·
transdermal (1)
onset:
None (55) ·
BP effect within 24 hours; full effect at 1-2 weeks (long half-life) (1) ·
IR 20 minutes; ER ~6 hours (1) ·
IV: 1-3 minutes (SVT termination); PO IR: 30-60 minutes; ER: hours (1) ·
IV: 3-7 minutes (rate control); PO IR: 30-60 minutes; ER: hours (1) ·
SL/spray: 1-3 minutes; IV: minutes; patch: 30-60 minutes (1) ·
SL: 2-5 minutes; PO mononitrate: 30-60 minutes (1) ·
~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (55) ·
24 hours (1) ·
6–10 h subjective; full pharmacologic effect considerably longer. (1) ·
IR 4-8 hours; ER 24 hours (1) ·
IR: 4-8 hours; ER: 24 hours (1) ·
IR: 6-8 hours; ER: 24 hours (1) ·
Mononitrate ER: 12-24 hours; dinitrate IR: 4-6 hours (1) ·
SL: 30 minutes; patch: 12-14 hours; IV continuous (1)
halflife:
None (55) ·
1-3 minutes (very short)'"`UNIQ--ref-00000C0F-QINU`"' (1) ·
2-5 hours (IR); ER formulations extend functional duration via osmotic/matrix release'"`UNIQ--ref-0000074D-QINU`"' (1) ·
3-4.5 hours (IR); 5-7 hours (ER; effective duration 24 hours via formulation)'"`UNIQ--ref-00000642-QINU`"' (1) ·
3-7 hours (IR); functional 24 hours (ER)'"`UNIQ--ref-00000A6B-QINU`"' (1) ·
30-50 hours'"`UNIQ--ref-00000078-QINU`"' (1) ·
Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) ·
Mononitrate ~5 hours; dinitrate ~1 hour'"`UNIQ--ref-00001461-QINU`"' (1)
bioavailability:
None (55) ·
64-90% (oral; not affected by food)'"`UNIQ--ref-00000079-QINU`"' (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) ·
Mononitrate ~100% (no first-pass; the principal advantage over dinitrate); dinitrate ~20%'"`UNIQ--ref-00001462-QINU`"' (1) ·
Not formally characterized in humans. (1) ·
~20-35% (oral; extensive first-pass via CYP3A4 with R/S enantiomer differences)'"`UNIQ--ref-00000A6C-QINU`"' (1) ·
~40% (oral; extensive first-pass via CYP3A4)'"`UNIQ--ref-00000643-QINU`"' (1) ·
~50% IR (extensive first-pass via CYP3A4); ER products release-rate-limited'"`UNIQ--ref-0000074E-QINU`"' (1)
pregnancy:
None (55) ·
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 data.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Limited data; alternative antihypertensives generally preferred. Crosses placenta.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Limited data; case series and registries suggest no major teratogenicity but other antihypertensives (labetalol, nifedipine) are typically preferred.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Limited data; labetalol/nifedipine generally preferred. Crosses placenta.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Oral nifedipine is one of the preferred agents for severe hypertension in pregnancy and for tocolysis in preterm labor.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</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.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1)
Showing below up to 62 results in range #1 to #62.