TEMARIL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TEMARIL (TEMARIL).
Temaril (trimeprazine tartrate and prednisolone) combines an antipruritic phenothiazine antihistamine with a corticosteroid. Trimeprazine blocks histamine H1 receptors, reducing pruritus and allergic reactions. Prednisolone suppresses inflammation via glucocorticoid receptor activation, inhibiting phospholipase A2 and cytokine production.
| Metabolism | Trimeprazine: Hepatic metabolism via CYP2D6 and other enzymes; active metabolites. Prednisolone: Hepatic metabolism primarily via 11β-hydroxysteroid dehydrogenase, conjugated and excreted renally. |
| Excretion | Primarily via kidneys as metabolites; unchanged drug accounts for <1%. Biliary/fecal excretion is minor. Approx. 90% recovered in urine within 24 hours. |
| Half-life | Terminal elimination half-life is 9–12 hours in adults; prolonged in hepatic impairment (up to 20 hours). Given TID dosing, steady state is reached within 2 days. |
| Protein binding | Approximately 90% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Vd is 8–13 L/kg, indicating extensive tissue distribution. Higher Vd in children (approx. 15 L/kg). |
| Bioavailability | Oral: 70–80% due to first-pass metabolism. Rectal: ~50% due to partial avoidance of first-pass. IM: ~100%. |
| Onset of Action | Oral: 30–60 minutes for antihistamine effect; peak effect at 2–3 hours. Rectal: 45–90 minutes. IM: 20–30 minutes. |
| Duration of Action | Antihistamine effect lasts 12–24 hours; antiemetic effect persists for 8–12 hours. Clinical duration may be shorter in children. |
2.5 mg orally twice daily or 5 mg orally at bedtime; maximum 10 mg/day.
| Dosage form | SYRUP |
| Renal impairment | No specific guidelines; use caution with severe renal impairment (CrCl <30 mL/min) due to risk of accumulation. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh class C). For Child-Pugh class B, reduce dose by 50%. No adjustment needed for Child-Pugh class A. |
| Pediatric use | Children 12 years and older: same as adult dose. Children 6-11 years: 2.5 mg at bedtime or 1.25 mg every 6 hours as needed; maximum 5 mg/day. Children <6 years: not recommended. |
| Geriatric use | Initiate at 2.5 mg once daily at bedtime; increase cautiously. Increased risk of sedation, confusion, and anticholinergic effects. Avoid in frail elderly. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TEMARIL (TEMARIL).
| Breastfeeding | Trimeprazine is excreted into breast milk in small amounts; M/P ratio unknown. Phenylephrine and phenylpropanolamine may reduce milk supply via vasoconstriction and have been associated with irritability and sleep disturbances in infants. Due to lack of safety data, TEMARIL is not recommended during breastfeeding. |
| Teratogenic Risk | TEMARIL (trimeprazine/phenylephrine/phenylpropanolamine combination) is generally not recommended in pregnancy, especially first trimester, due to potential teratogenic effects from antihistamine and sympathomimetic components. Data are limited; however, phenothiazines have been associated with congenital malformations when used early in pregnancy. In second and third trimesters, risk of maternal and fetal tachycardia, uterine contractions, and reduced placental perfusion exists due to vasoconstrictors. Avoid use unless benefit outweighs risk. |
■ FDA Black Box Warning
No FDA black box warning
| Serious Effects |
["Hypersensitivity to trimeprazine, prednisolone, or other phenothiazines","Systemic fungal infections (corticosteroid contraindication)","Concurrent use with MAOIs (trimeprazine contraindication)","Pregnancy and lactation (contraindicated unless potential benefit outweighs risk)","Pre-existing gastrointestinal ulceration or severe hepatic impairment"]
| Precautions | ["Corticosteroid-related: adrenal suppression, increased susceptibility to infections, gastrointestinal ulceration, osteoporosis, and growth suppression in young animals","Phenothiazine antihistamine: potential for sedation, extrapyramidal symptoms, anticholinergic effects (e.g., dry mouth, urinary retention)","Use with caution in animals with diabetes mellitus, heart failure, or renal disease","Avoid abrupt discontinuation after prolonged use to prevent adrenal insufficiency"] |
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| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and signs of uterine hypertonicity. Fetal heart rate monitoring recommended if used near term. Assess for neonatal respiratory depression, sedation, and feeding difficulties after delivery. |
| Fertility Effects | No specific human data. Antihistamines may theoretically alter ovulation via anticholinergic effects; sympathomimetics can affect hormonal balance. Animal studies have shown reduced fertility at high doses. Clinical significance unknown. |