CARTROL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CARTROL (CARTROL).
CARTROL is a beta-1 selective adrenergic receptor antagonist. It inhibits the effects of catecholamines on beta-1 receptors in the heart, reducing heart rate, myocardial contractility, and blood pressure.
| Metabolism | Primarily metabolized by CYP2D6 to active metabolites. Minor pathways: CYP1A2 and glucuronidation. |
| Excretion | Primarily renal excretion (approx. 70% unchanged drug), with 20% biliary/fecal, and 10% metabolism to inactive metabolites. |
| Half-life | Terminal elimination half-life is 6–8 hours in normal renal function; prolonged to 20–40 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 25–30% bound to albumin. |
| Volume of Distribution | 1.5–2.0 L/kg, indicating extensive extravascular distribution. |
| Bioavailability | Oral: 60–80% (extensive first-pass metabolism). IM: 90–100%. |
| Onset of Action | IV: 1–2 minutes; IM: 5–10 minutes; Oral: 30–60 minutes. |
| Duration of Action | IV bolus: 1–2 hours; IM: 2–4 hours; Oral: 4–6 hours. Extended-release: 12–24 hours. |
Adults: 2.5 mg orally twice daily, titrated up to maximum 10 mg twice daily.
| Dosage form | TABLET |
| Renal impairment | GFR 30-89 mL/min: no adjustment. GFR <30 mL/min: use 1.25 mg twice daily. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: 1.25 mg twice daily. Child-Pugh C: contraindicated. |
| Pediatric use | Not approved for pediatric use; no established dosing. |
| Geriatric use | Start at 1.25 mg twice daily; titrate cautiously due to increased sensitivity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CARTROL (CARTROL).
| Breastfeeding | No data available on the excretion of CARTROL in human breast milk. The molecular weight is low enough to suggest potential transfer. Due to the theoretical risk of neonatal adverse effects (hypotension, renal dysfunction), breastfeeding is not recommended during therapy. M/P ratio unknown. |
| Teratogenic Risk | CARTROL is an angiotensin II receptor blocker (ARB). Based on its mechanism of action and class effects, it carries a risk of fetal renal dysfunction, oligohydramnios, skull ossification defects, and hypotension in the fetus when used during the second and third trimesters. First trimester exposure is associated with a low risk of major congenital malformations, but potential fetotoxicity increases after 20 weeks gestation. Use is contraindicated in pregnancy; discontinue as soon as pregnancy is detected. |
■ FDA Black Box Warning
Do not abruptly discontinue therapy as this may exacerbate angina and increase risk of myocardial infarction. Taper dose over 1-2 weeks if discontinuation is needed.
| Serious Effects |
Hypersensitivity to CARTROL or any component; cardiogenic shock; overt cardiac failure; second- or third-degree AV block; severe bradycardia; sick sinus syndrome (without pacemaker); severe peripheral arterial disease; history of bronchial asthma or severe COPD; severe hepatic impairment.
| Precautions | May mask symptoms of hypoglycemia and hyperthyroidism. Use with caution in patients with bronchospastic diseases, peripheral vascular disease, diabetes, and pheochromocytoma. Monitor renal function in patients with severe renal impairment. Avoid use with calcium channel blockers with negative inotropic effects. |
| Food/Dietary | Cartrol may be taken with or without food. No specific food interactions are documented. Avoid excessive alcohol intake as it may potentiate hypotensive effects. |
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| Fetal Monitoring | Monitor maternal blood pressure, renal function (serum creatinine, BUN), and serum electrolytes (potassium) monthly. If inadvertently used during pregnancy, perform serial ultrasound assessments of amniotic fluid index and fetal renal function. Fetal growth monitoring recommended after 20 weeks gestation. |
| Fertility Effects | No direct human studies on fertility. In animal studies, ARBs have been associated with reduced sperm motility and testicular atrophy at high doses. Clinical relevance unknown, but reversible upon discontinuation. No evidence of impairment of female fertility. |
| Clinical Pearls | Cartrol (carteolol) is a non-selective beta-blocker with intrinsic sympathomimetic activity (ISA). It is primarily used for hypertension and glaucoma (ophthalmic solution). Clinicians should monitor heart rate and blood pressure, as bradycardia and hypotension can occur. Abrupt withdrawal may precipitate angina or myocardial infarction in patients with ischemic heart disease. In glaucoma, note that ophthalmic carteolol can produce systemic effects; patients with asthma or COPD may experience bronchospasm. Use with caution in diabetes because beta-blockers can mask hypoglycemia symptoms. Due to ISA, carteolol may cause less resting bradycardia than other beta-blockers. |
| Patient Advice | Take this medication exactly as prescribed, with or without food. · Do not stop taking this medication abruptly; it may worsen chest pain or increase risk of heart attack. · If you have diabetes, monitor blood sugar closely as this drug may mask signs of low blood sugar. · Avoid activities requiring alertness until you know how this drug affects you, as dizziness or fatigue may occur. · If using eye drops, wash hands before and after, and avoid touching the dropper tip to any surface. · Report slow heartbeat, shortness of breath, swelling of extremities, or unusual weight gain to your healthcare provider. · Do not use over-the-counter cold or allergy medications without consulting your doctor, as they may interact. |