PMB 200
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PMB 200 (PMB 200).
PMB 200 is a fixed-dose combination of an angiotensin II receptor blocker (ARB) and a calcium channel blocker (CCB). The ARB component blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively antagonizing the AT1 receptor, leading to vasodilation and reduced blood pressure. The CCB component inhibits the influx of calcium ions through L-type channels in vascular smooth muscle and cardiac muscle, resulting in peripheral vasodilation and decreased blood pressure.
| Metabolism | The ARB component is metabolized primarily by CYP2C9 and to a lesser extent by CYP3A4. The CCB component is metabolized by CYP3A4. |
| Excretion | Renal (80% unchanged, 15% as glucuronide conjugate), biliary/fecal (5%) |
| Half-life | Terminal elimination half-life 12 hours (range 10-14 h) in adults with normal renal function; prolonged to 24-36 h in moderate renal impairment (CrCl 30-50 mL/min), necessitating dose adjustment |
| Protein binding | 98% (primarily to albumin, minor binding to alpha-1-acid glycoprotein) |
| Volume of Distribution | 0.3 L/kg (range 0.25-0.35 L/kg). Indicates distribution primarily into extracellular fluid; low Vd reflects limited tissue penetration with high plasma protein binding |
| Bioavailability | Oral: 75% (range 65-85%) due to first-pass metabolism; Rectal: 60% (variable, 40-80%); Intramuscular: 90% (well-absorbed) |
| Onset of Action | Intravenous: 2-5 minutes; Oral: 30-60 minutes (fasting), up to 2 hours with food |
| Duration of Action | Intravenous: 4-6 hours; Oral: 6-8 hours (dose-dependent, shorter at lower doses). Duration may be extended in hepatic impairment due to reduced clearance |
| Molecular Weight | 425.5 |
2.5 mg orally once daily, increased to 5 mg after 2 weeks if tolerated; maximum 10 mg once daily.
| Dosage form | TABLET |
| Renal impairment | eGFR 30-50: 2.5 mg once daily; eGFR <30: not recommended. |
| Liver impairment | Child-Pugh A: 2.5 mg once daily; Child-Pugh B: not recommended; Child-Pugh C: contraindicated. |
| Pediatric use | Not approved for patients <18 years; safety and efficacy not established. |
| Geriatric use | Initial dose 2.5 mg once daily; increase cautiously; monitor for hypotension and renal function. |
| 1st trimester | Avoid use due to potential teratogenic effects based on animal studies. |
| 2nd trimester | Use only if potential benefit justifies risk to fetus; limited human data. |
| 3rd trimester | Avoid use near term due to risk of adverse effects (e.g., premature closure of ductus arteriosus). |
Clinical note
Comprehensive clinical and safety monograph for PMB 200 (PMB 200).
| Placental transfer | Crosses placenta (human data limited; animal studies demonstrate transfer). |
| Breastfeeding | Excreted in human milk in low amounts; consider risk vs benefit. Monitor infant for adverse effects. |
| Lactation Rating |
■ FDA Black Box Warning
No FDA black box warnings.
| Serious Effects |
Hypersensitivity to PMB 200 or any componentSevere hepatic impairmentConcurrent use with MAO inhibitors
| Precautions | Avoid use in pregnancy (fetal toxicity), Symptomatic hypotension in volume-depleted patients, Monitor renal function and serum potassium, Peripheral edema, particularly with high doses of the CCB component |
| Food/Dietary | Avoid high-potassium foods (bananas, oranges, potatoes, tomatoes, spinach, salt substitutes). Limit sodium intake to <2 g/day. Grapefruit and grapefruit juice may increase drug levels; avoid consumption. |
| Clinical Pearls |
Loading safety data…
| L3 – Moderately Safe |
| Teratogenic Risk | First trimester: Increased risk of spontaneous abortion and major malformations including neural tube defects, facial clefts, and cardiac anomalies. Second/third trimester: Risk of fetal growth restriction, oligohydramnios, and premature closure of ductus arteriosus. Late third trimester: Potential neonatal complications include persistent pulmonary hypertension and renal impairment. |
| Fetal Monitoring | Maternal: Monitor blood pressure, renal function, liver enzymes, and signs of hypersensitivity. Fetal: Serial ultrasound for growth, amniotic fluid index, and ductus arteriosus Doppler. Neonatal: Observe for respiratory distress, hypoglycemia, and withdrawal symptoms. |
| Fertility Effects | May impair fertility in both males and females based on animal studies. Reversible upon discontinuation in most cases. Sperm abnormalities and menstrual irregularities reported. |
| PMB 200 (Prescription Medication B 200) is a high-dose formulation; start at lowest effective dose and titrate slowly. Monitor renal function and electrolytes (especially potassium) monthly. Avoid use with NSAIDs due to increased nephrotoxicity. Discontinue if GFR falls below 30 mL/min. |
| Patient Advice | Take exactly as prescribed; do not double dose if missed. · Report any signs of hyperkalemia (muscle weakness, palpitations, numbness). · Maintain adequate hydration; avoid dehydration. · Inform all healthcare providers you are taking PMB 200. · Do not stop abruptly; may require taper. |