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 |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PMB 200 (PMB 200).
| Breastfeeding | Excreted in breast milk; M/P ratio unknown. Potential adverse effects in nursing infants. Breastfeeding not recommended during therapy. |
| 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. |
■ FDA Black Box Warning
No FDA black box warnings.
| Serious Effects |
["Concomitant use with aliskiren in patients with diabetes","History of angioedema related to previous ARB therapy","Severe aortic stenosis","Pregnancy"]
| 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"] |
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| 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. |