Formulary
Tirzepatide: Indications, Dosing, Side Effects and Interactions
Tirzepatide is a long-acting GIP (glucose-dependent insulinotropic polypeptide) receptor and GLP-1 (glucagon-like peptide-1) receptor agonist that increases...
MedNext Academy | 4 min read
Tirzepatide: Indications, Dosing, Side Effects and Interactions
Tirzepatide is a long-acting GIP (glucose-dependent insulinotropic polypeptide) receptor and GLP-1 (glucagon-like peptide-1) receptor agonist that increases...
Drug action
Tirzepatide is a long-acting GIP (glucose-dependent insulinotropic polypeptide) receptor and GLP-1 (glucagon-like peptide-1) receptor agonist that increases insulin sensitivity and secretion, suppresses glucagon secretion, and slows gastric emptying.
Indications and dose
**Type 2 diabetes mellitus as monotherapy [if metformin inappropriate],Type 2 diabetes mellitus in combination with other antidiabetic drugs (including insulin) [if existing treatment fails to achieve adequate glycaemic control]**
- **Adult** (By Subcutaneous Injection): Initially 2.5 mg once weekly for 4 weeks, then increased to 5 mg once weekly for at least 4 weeks, then increased if necessary up to 15 mg once weekly, dose to be increased in steps of 2.5 mg at intervals of at least 4 weeks.
**Weight management [in conjunction with dietary measures and increased physical activity in individuals with a BMI of 30 kg/m2or more, or in individuals with a BMI of 27 kg/m2or more in the presence of at least one weight-related co-morbidity]**
- **Adult** (By Subcutaneous Injection): Weight management [in conjunction with dietary measures and increased physical activity in individuals with a BMI of 30 kg/m 2 or more, or in individuals with a BMI of 27 kg/m 2 or more in the presence of at least one weight-related co-morbidity] Initially 2.5 mg once weekly for 4 weeks, then increased to 5 mg once weekly for at least 4 weeks, then increased if necessary up to 15 mg once weekly, dose to be increased in steps of 2.5 mg at intervals of at least 4 weeks. Assess benefit of continuing treatment if at least 5% of initial body-weight has not been lost after 6 months at highest tolerated dose.
Cautions
Delayed gastric emptying; diabetic retinopathy; general anaesthesia or deep sedation (risk of pulmonary aspiration due to delayed gastric emptying); history of pancreatitis; severe gastro-intestinal disease Cautions, further information Delayed gastric emptying Tirzepatide delays gastric emptying, particularly following the first dose. This has the potential to slow the rate of absorption of concomitant oral medicines. The risk of a delayed effect should be considered for oral medicines where a rapid onset of action is important. Monitor patients on oral medicines with a narrow therapeutic index, especially at the start of tirzepatide treatment and after dose increases. M See also Conception and Contraception , below.
Side effects
Common or very common Alopecia; appetite decreased (in patients with type 2 diabetes); asthenia; burping; constipation; diarrhoea; dizziness; gastrointestinal discomfort; gastrointestinal disorders; hypersensitivity; hypotension; lethargy; malaise; nausea; vomiting Uncommon Gallbladder disorders; pancreatitis acute; taste altered; weight decreased (in patients with type 2 diabetes) Rare or very rare Angioedema Frequency not known Hypoglycaemia Side-effects, further information Discontinue if symptoms of acute pancreatitis occur, such as persistent, severe abdominal pain. If pancreatitis confirmed, do not restart treatment.
Interactions
**Other interactions (14):**
- Tirzepatide delays gastric emptying and thereby has the potential to impact the rate of absorption of concomitantly administered oral medicinal products.
- This effect, resulting in decreased C max and a delayed t max , is most pronounced at the time of tirzepatide treatment initiation.
- Based on the results from a study with paracetamol, which was used as a model medicinal product to evaluate the effect of tirzepatide on gastric emptying, no dose adjustments are expected to be...
- However, it is recommended to monitor patients on oral medicinal products with a narrow therapeutic index (e.g., warfarin, digoxin), especially at initiation of -tirzepatide treatment and following...
- Paracetamol No dose adjustment of paracetamol is necessary when administered with tirzepatide.
- Following a 5 mg single dose of tirzepatide, the maximum plasma concentration (C max ) of paracetamol was reduced by 50 %, and the median (t max ) was delayed by 1 hour.
Pregnancy
Avoid-toxicity in animal studies. M
Breast feeding
Specialist sources indicate use with caution-no information available. Large molecular weight suggests limited excretion into milk and drug molecule likely to be partially destroyed in the infant's gastro-intestinal tract.
Hepatic impairment
Mounjaro Kwikpen with caution (potential risk of metabolic acidosis due to accumulation of benzyl alcohol excipient over time). M
Renal impairment
Mounjaro Kwikpen with caution (potential risk of metabolic acidosis due to accumulation of benzyl alcohol excipient over time). M
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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