Tirzepatide
Regulatory sources consulted
- EMA/H/C/005620
- https://www.ema.europa.eu/en/medicines/human/EPAR/mounjaro
- PMID:40865172
- PMID:41638556
- PMID:40716192
- PMID:40466247
- AEMPS CIMA · nº registro 1221685055 ↗
- EMA EPAR · EMEA/H/C/005620 ↗
- RxNorm rxcui 2601723 ↗
- PubMed PMID:40466247 ↗
- PubMed PMID:40865172 ↗
- PubMed PMID:40716192 ↗
- PubMed PMID:41638556 ↗
Approved indications
- Treatment of adults with insufficiently controlled type 2 diabetes mellitus as an adjunct to diet and exercise, as monotherapy when metformin is considered inappropriate due to intolerance or contraindications, or in addition to other medicinal products for the treatment of diabetes.
- As an adjunct to a reduced-calorie diet and increased physical activity for weight management, including weight loss and weight maintenance, in adults with an initial Body Mass Index (BMI) of ≥ 30 kg/m² (obesity) or ≥ 27 kg/m² to < 30 kg/m² (overweight) in the presence of at least one weight-related comorbid condition (e.g., hypertension, dyslipidaemia, obstructive sleep apnoea, cardiovascular disease, prediabetes, or type 2 diabetes mellitus).
Contraindications
Absolute
- Hypersensitivity to the active substance or to any of the excipients.
- Personal or family history of medullary thyroid carcinoma (MTC) or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN 2).
Clinical warnings
- Boxed warning · Thyroid C-cell Tumors: C-cell tumors have been observed in rodent studies, but the relevance to humans is unknown. Contraindicated in patients with a personal or family history of MTC or MEN 2. — FDA
- Major warning · Pancreatitis: Acute pancreatitis has been reported. Patients should be informed of the characteristic symptoms. If pancreatitis is suspected, treatment should be discontinued. — EMA
Drug interactions
- ModerateOral contraceptivesG03A
Mechanism: Delayed gastric emptying, which may reduce the rate and extent of absorption of oral contraceptives.
Recommendation: Advise patients to use a non-oral contraceptive method or an additional barrier method for 4 weeks after initiation and for 4 weeks after each dose escalation.
EMA SPC
- ModerateWarfarinB01AA03
Mechanism: Potential alteration of absorption due to delayed gastric emptying. Although studies did not show a clinically relevant effect on warfarin AUC or Cmax, monitoring is warranted.
Recommendation: Monitor INR more frequently upon initiation or dose escalation of tirzepatide in patients treated with warfarin or other coumarin derivatives.
EMA SPC
Adverse events
Common (≥1%)
nausea · diarrhea · decreased appetite · vomiting · constipation · dyspepsia · abdominal pain
Rare but serious
acute pancreatitis · cholelithiasis · cholecystitis · gastroparesis · severe hypersensitivity reactions · acute kidney injury · ileus
Pregnancy and lactation
Should not be used during pregnancy. It is recommended that women of childbearing potential use contraception. Treatment should be discontinued at least 1 month before a planned pregnancy. Should not be used during breast-feeding.
Recent literature (PubMed)
Revisión sobre el tratamiento de la obesidad que destaca la nueva era de fármacos de segunda generación. Señala específicamente que la tirzepatida, un agonista dual del receptor GLP-1/GIP, logra una pérdida de peso de hasta el 22,5% en las dosis más altas, acercándose a la eficacia de la cirugía bariátrica.
Documento de consenso que actualiza el manejo de la insuficiencia cardíaca con fracción de eyección preservada (IC-FEp). Menciona la tirzepatida como una de las nuevas evidencias de beneficio clínico en esta patología, junto a los iSGLT2, finerenona y semaglutida.
Analiza el uso de agonistas GLP-1 y coagonistas GIP/GLP-1 como la tirzepatida para la obesidad en poblaciones especiales (adolescentes y ancianos). Destaca que estos fármacos ofrecen beneficios significativos en la reducción de peso, aunque con consideraciones de seguridad particulares para cada grupo de edad.
Revisión de los mecanismos de acción de los medicamentos basados en GLP-1 para la obesidad. Explica cómo los multiagonistas, como los que combinan la acción de GIP (ej. tirzepatida), potencian y complementan los efectos del GLP-1 para lograr una mayor pérdida de peso y beneficios metabólicos adicionales.