CODIMAL-L.A. 12
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CODIMAL-L.A. 12 (CODIMAL-L.A. 12).
Codimal-L.A. 12 contains chlorpheniramine, a histamine H1 receptor antagonist, and pseudoephedrine, a sympathomimetic amine that directly stimulates alpha-adrenergic receptors. Chlorpheniramine competitively blocks histamine at H1 receptors, reducing allergic symptoms. Pseudoephedrine causes vasoconstriction via alpha-1 adrenergic receptor activation, leading to nasal decongestion.
| Metabolism | Chlorpheniramine is extensively metabolized in the liver via CYP450 enzymes, primarily CYP2D6. Pseudoephedrine is partially metabolized in the liver by N-demethylation, with about 70-90% excreted unchanged in urine. |
| Excretion | Renal: 90% (unchanged drug). Biliary/fecal: <10%. |
| Half-life | 12 hours (terminal); supports once-daily dosing, steady-state in 2-3 days. |
| Protein binding | 60% (primarily albumin). |
| Volume of Distribution | 0.8 L/kg; indicates moderate tissue distribution. |
| Bioavailability | Oral: 90% (sustained release). |
| Onset of Action | Oral: 30-60 minutes. |
| Duration of Action | 12 hours (sustained release formulation). |
One tablet orally every 12 hours. Each tablet contains 25 mg phenylpropanolamine HCl and 4 mg chlorpheniramine maleate.
| Dosage form | CAPSULE, EXTENDED RELEASE |
| Renal impairment | Avoid use if GFR < 30 mL/min due to anticholinergic effects and reduced clearance; use with caution if GFR 30-60 mL/min. |
| Liver impairment | Contraindicated in Child-Pugh C cirrhosis; reduce dose by 50% in Child-Pugh B; no adjustment in Child-Pugh A. |
| Pediatric use | Not recommended for children under 12 years due to safety concerns; for age 12-18, adult dosing may be considered with caution. |
| Geriatric use | Initiate at half the adult dose (0.5 tablet every 12 hours) due to increased sensitivity to anticholinergic and pressor effects; monitor for sedation and hypertension. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CODIMAL-L.A. 12 (CODIMAL-L.A. 12).
| Breastfeeding | Codeine is excreted into breast milk with a relative infant dose of approximately 2-7% of weight-adjusted maternal dose; M/P ratio unknown. Risk of infant opioid toxicity, especially in CYP2D6 ultra-rapid metabolizers. Chlorpheniramine and phenylephrine may reduce milk supply or cause infant irritability. Avoid during breastfeeding. |
| Teratogenic Risk | First trimester: Not recommended due to possible association with cardiovascular malformations and neural tube defects from antihistamine component (chlorpheniramine). Second and third trimesters: Avoid due to risk of premature closure of ductus arteriosus from sympathomimetic (phenylephrine) and potential neonatal respiratory depression from codeine. Codeine is contraindicated due to risk of neonatal opioid withdrawal syndrome and respiratory depression. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to any component","Severe hypertension or coronary artery disease","Concomitant use with MAO inhibitors (within 14 days)","Narrow-angle glaucoma","Urinary retention","Acute myocardial infarction"]
| Precautions | ["Cardiovascular effects: caution in hypertension, ischemic heart disease, arrhythmias","CNS stimulation: insomnia, anxiety, tremor","Anticholinergic effects: urinary retention, glaucoma exacerbation, dry mouth","Caution in elderly and patients with prostatic hypertrophy","Avoid in severe renal impairment"] |
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| Fetal Monitoring | Monitor fetal heart rate and uterine activity if used near term. Assess for neonatal respiratory depression, sedation, and withdrawal symptoms after delivery. Monitor maternal blood pressure and heart rate due to sympathomimetic effects. |
| Fertility Effects | Codeine may impair spermatogenesis and reduce sperm count. Antihistamines may cause transient menstrual irregularities. No known effect on female fertility from phenylephrine. Overall, limited data suggest potential reversible impairment of male fertility. |