NITROGLYCERIN IN DEXTROSE 5%
Clinical safety rating
cautionComprehensive clinical and safety monograph for NITROGLYCERIN IN DEXTROSE 5% (NITROGLYCERIN IN DEXTROSE 5%).
Nitroglycerin is a vasodilator that relaxes vascular smooth muscle via the release of nitric oxide (NO), which activates guanylate cyclase, increasing cGMP levels and causing venous and arterial dilation.
| Metabolism | Extensively metabolized in the liver by glutathione-dependent organic nitrate reductase, and to a lesser extent via cytochrome P450 (CYP3A4). Primary metabolite is 1,2-glyceryl dinitrate (active). |
| Excretion | Renal: ~33% as intact drug; hepatic metabolism accounts for >90% of clearance; biliary/fecal: negligible. |
| Half-life | Terminal elimination half-life: 1–4 minutes; clinical context: rapid clearance due to extensive metabolism by glutathione-S-transferase and glutathionylation. |
| Protein binding | ~60% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd: 0.3 L/kg; reflects distribution into vascular smooth muscle and minimal tissue penetration. |
| Bioavailability | Intravenous: 100%; sublingual: ~40% (first-pass hepatic metabolism); oral: <10% due to extensive first-pass effect. |
| Onset of Action | Intravenous: 1–2 minutes; onset immediate with bolus. |
| Duration of Action | Intravenous: 3–5 minutes after infusion cessation; continuous infusion required for sustained effect. |
| Molecular Weight | 227.09 |
Intravenous infusion: Initial 5 mcg/min, titrate by 5 mcg/min every 3-5 minutes to hemodynamic effect; usual maintenance 10-200 mcg/min. Sublingual: 0.3-0.6 mg every 5 minutes up to 3 doses. Topical: 1-2 inches every 8 hours.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment required for renal impairment; monitor for volume status and hypotension. |
| Liver impairment | Child-Pugh Class A: No adjustment. Class B: Reduce initial dose by 50%. Class C: Avoid use or reduce initial dose by 75%. |
| Pediatric use | Not FDA-approved for pediatric use. Limited data: IV infusion 0.25-0.5 mcg/kg/min, titrate to effect; max 5 mcg/kg/min. |
| Geriatric use | Lower initial doses recommended due to increased sensitivity; start at 5 mcg/min IV or 0.3 mg sublingual; monitor for hypotension. |
| 1st trimester | Limited human data; use only if clearly needed and benefits outweigh risks. |
| 2nd trimester | Use with caution; may cause maternal hypotension and reduce placental perfusion. |
| 3rd trimester | Avoid near term due to risk of fetal bradycardia, hypotension, and methemoglobinemia. |
Clinical note
Comprehensive clinical and safety monograph for NITROGLYCERIN IN DEXTROSE 5% (NITROGLYCERIN IN DEXTROSE 5%).
| Placental transfer | Nitroglycerin is a small molecule that crosses the placenta; fetal exposure confirmed in animal and limited human studies. |
| Breastfeeding | Trace amounts excreted in breast milk; unlikely to cause adverse effects in infant. Use with caution in breastfeeding women with hypotension or vascular compromise. |
| Lactation Rating | L2 (Probably Compatible) |
| Teratogenic Risk | Nitroglycerin is generally considered to have low teratogenic potential. In the first trimester, there is no evidence of increased risk of major congenital malformations from human data. However, animal studies are insufficient to rule out risk. During the second and third trimesters, nitroglycerin is used for tocolysis and management of hypertensive emergencies without documented fetal harm, but potential for maternal hypotension leading to reduced uteroplacental perfusion exists. Overall, FDA assigns category C (risk cannot be ruled out). |
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and oxygen saturation continuously during infusion. Fetal heart rate monitoring is recommended during use for preterm labor or hypertensive emergencies. Assess for maternal hypotension (systolic BP <90 mmHg) and signs of fetal distress. |
| Fertility Effects | No well-controlled studies on fertility in humans. Animal studies have not shown impaired fertility at clinically relevant doses. Theoretical concerns about reduced uterine blood flow due to vasodilation have not been substantiated in fertility assessments. |
■ FDA Black Box Warning
NOT available in this formulation. Nitroglycerin products do not carry a black box warning.
| Serious Effects |
Hypersensitivity to nitroglycerin or any componentSevere anemiaIncreased intracranial pressure (e.g., head trauma, cerebral hemorrhage)Constrictive pericarditisPericardial tamponadeConcomitant use with phosphodiesterase-5 inhibitors (e.g., sildenafil, tadalafil)Circulatory collapse or cardiogenic shockAcute myocardial infarction with low left ventricular filling pressure
| Precautions | Hypotension (severe hypotension may occur, especially with hypovolemia), Bradycardia and paradoxical tachycardia, Increased intracranial pressure (use cautiously in head trauma or intracranial hemorrhage), Tolerance to nitrates with prolonged use (intermittent dosing recommended), Methemoglobinemia (rare, risk with high doses or prolonged infusion), Drug interactions with phosphodiesterase inhibitors (e.g., sildenafil) causing severe hypotension |
| Food/Dietary | Avoid alcohol; may cause severe hypotension and reflex tachycardia. No other significant food interactions. |
| Clinical Pearls | For IV nitroglycerin in D5W, use non-PVC tubing (light-sensitive) and inline filter; avoid abrupt discontinuation to prevent rebound hypertension; titrate to chest pain relief or hemodynamic parameters; monitor for hypotension and bradycardia; tolerance may develop after 24 hours of continuous infusion. |
| Patient Advice | Report any chest pain, severe headache, or dizziness immediately. · Avoid alcohol consumption while on this medication. · Do not stop infusion suddenly without medical supervision. · Remain lying down if dizzy or lightheaded. · Inform all healthcare providers of nitroglycerin use. |
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