Tirzepatide
Pharmacokinetics
| Half-life | 120 hours |
| Tmax | 24 h |
| Bioavailability | 80 % (approx) |
| Protein Binding | 99 % |
| Volume of Distribution | 0.1 L/kg (approx) |
| Clearance Route | other |
| Active Metabolites | no |
| Notes | Long half-life (~5 days) enables once-weekly dosing; eliminated by proteolytic cleavage, not CYP-dependent. |
⚠️ Safety & Warnings
Severity: Moderate
Adverse Effects:
Nausea, vomiting, diarrhea, decreased appetite, delayed gastric emptying
Contraindications:
Personal or family history of medullary thyroid carcinoma, MEN2
Precautions:
Risk of hypoglycemia when combined with insulin or sulfonylureas; slow dose escalation reduces GI effects
Note :: Tirzepatide is an agonist of the receptors of two insulin sensitizing polypeptides, GIP (glucose-dependent insulinotropic polypeptide) and GLP-1 (glucagon-like peptide 1), that is used as therapy of type 2 diabetes, obstructive sleep apnea, and obesity. Tirzepatide has been linked to minimal instances of elevations in serum aminotransferase levels during therapy and rare episodes of clinically apparent liver injury.