Drug intelligence / Profile preview

Methylprednisolone + Thiethylperazine

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

The combination of methylprednisolone and thiethylperazine is primarily used as an antiemetic regimen for managing chemotherapy-induced nausea and vomiting. This combination has been studied in clinical trials and shown to be effective, particularly for patients receiving chemotherapy for breast cancer. ## Pharmacological Properties **Methylprednisolone** is a corticosteroid that works by calming down the immune system and preventing certain substances in the body from causing inflammation[5]. It's used to treat various conditions including allergies, inflammation, immune system disorders, and certain types of cancer[9]. **Thiethylperazine** is a phenothiazine antiemetic that blocks dopamine receptors in the chemoreceptor trigger zone (CTZ) and the vomiting center in the brain[7]. By inhibiting the transmission of nausea signals, it helps alleviate symptoms of nausea and vomiting. ## Clinical Efficacy In a multicenter, randomized, double-blind, cross-over trial involving 46 women with breast cancer treated with adjuvant FAC (fluorouracil, doxorubicin and cyclophosphamide), the combination of thiethylperazine plus methylprednisolone was significantly better than thiethylperazine plus placebo in reducing vomiting (p < 0.01) and nausea (p < 0.02)[1]. The complete protection rate against vomiting was 36% for the combination compared to 18% for thiethylperazine alone, and the percentage of patients with no or slight nausea was 59% versus 27% respectively[1]. Patient preference after cross-over was strongly in favor of the combination (70% versus 13%, p < 0.001)[1]. ## Dosage and Administration Based on the available information: - Methylprednisolone: 250 mg intravenous × 2 doses - Thiethylperazine: 6.5 mg oral every 8 hours × 3 days ## Side Effects The combination may cause side effects associated with each individual component: **Methylprednisolone side effects**: - Headache - Increased appetite - Skin changes - Fluid retention - Elevated blood sugar or blood pressure[5] **Thiethylperazine side effects**: - Sedation, dizziness, headache - Extrapyramidal reactions (rare, <1% of patients) - Dry mouth and nose - Altered taste sensation - Hypotension during intravenous administration - Blurred vision[8] ## Precautions and Contraindications Care should be taken when using this combination in patients with: - Liver disease - Cardiovascular conditions - History of seizures - Known hypersensitivity to either component An anaphylactic reaction to thiethylperazine has been reported in at least one case[8]. This combination appears to be particularly useful in managing chemotherapy-induced nausea and vomiting, with evidence suggesting it provides better antiemetic control than thiethylperazine alone.

02

Targets

DRD4 (Dopamine D4 Receptor)HRH1 (Histamine H1 Receptor)ADRA1A (α1A)HTR2A (Serotonin receptor 5-HT2A)mAChR (Muscarinic acetylcholine receptors)DRD1 (Dopamine D1 Receptor)HTR2C (5-hydroxytryptamine 2C receptor)DRD2 (Dopamine D2 Receptor)GR (Glucocorticoid receptor)

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