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    Tirzepatide - the new antidiabetic drug

    Chronic Conditions
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      Bikas Aryan last edited by

      How does the new antidiabetic drug Tirzepatide work ? what are the contraindications and side effects?

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        Sanjeev Tiwari @Bikas Aryan last edited by

        @bikas-aryan harmacology
        Mechanism of Action
        Dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist

        GIP is an incretin hormone that induces insulin secretion in response to a meal (primarily by hyperosmolarity of glucose in the duodenum) to facilitate the metabolism of carbohydrates, fats, and proteins

        GLP-1 receptor agonists increase insulin secretion in the presence of elevated blood glucose, suppress glucagon postprandially, delay gastric emptying to decrease postprandial glucose, and decrease glucagon secretion

        Pharmacodynamic effects observed include lower fasting and postprandial glucose concentration, decreased food intake, and reduced body weight

        Absorption
        Bioavailability: 80%

        Peak plasma concentration: 8-72 hr

        Steady-state achieved: 4 weeks

        Distribution
        Protein bound: 99% (primarily to albumin)

        Vd: 10.3 L

        Metabolism
        Metabolized by proteolytic cleavage of the peptide backbone, beta-oxidation of the C20 fatty diacid moiety, and amide hydrolysis

        Elimination
        Half-life: ~5 days

        Clearance: 0.061 L/hr

        Excretion: Metabolites via urine and feces

        Contraindications
        Personal or family history of MTC or in patients with multiple endocrine neoplasia syndrome type 2

        Known hypersensitivity to tirzepatide or to any of the product components

        Cautions
        On the basis of findings in rats and mice, may cause thyroid C-cell tumors, including MTC, in humans; human relevance of tirzepatide-induced rodent thyroid C-cell tumors has not been determined

        Acute pancreatitis, including fatal and non-fatal hemorrhagic or necrotizing pancreatitis, observed in patients treated with GLP-1 receptor agonists; after initiating, monitor for signs and symptoms of pancreatitis (eg, persistent severe abdominal pain, which sometimes radiates to the back and may or may not be accompanied by vomiting); if pancreatitis suspected, discontinue and do not restart if confirmed

        Rapid improvement in glucose control associated with temporary worsening of diabetic retinopathy; tirzepatide has not been studied in patients with nonproliferative diabetic retinopathy requiring acute therapy, proliferative diabetic retinopathy, or diabetic macular edema; monitor patients with a history of diabetic retinopathy

        Gastrointestinal (GI) adverse reactions, sometimes severe, reported; has not been studied in patients with severe GI disease, including severe gastroparesis, and is not recommended in these patients

        Acute gallbladder disease (eg, cholelithiasis, cholecystitis) reported in GLP-1 receptor agonist trials and postmarketing surveillance; if suspected, gallbladder studies and appropriate clinical follow-up are indicated

        Kidney injury
        Acute kidney injury and worsening of chronic renal failure, which may sometimes require hemodialysis in patients treated with GLP-1 receptor agonists, has been described
        Most reported events occurred in patients who had experienced nausea, vomiting, diarrhea, or dehydration
        Events also reported in patients without known underlying renal disease
        Monitor renal function when initiating or escalating doses in patients reporting severe adverse GI reactions
        Hypersensitivity
        Serious hypersensitivity reactions reported with GLP-1 receptor agonists; caution in patients with history of angioedema or anaphylaxis with a GLP-1 receptor agonist
        Unknown whether such patients will be predisposed to these reactions with tirzepatide
        If hypersensitivity reactions occur, discontinue treatment, treat promptly, and monitor until signs and symptoms resolve
        Drug interaction overview
        Insulin secretagogues or insulin
        May require dosage modification
        Coadministration with insulin secretagogues (eg, sulfonylureas) or insulin may increase risk of hypoglycemia
        Consider lower dose of secretagogue or insulin to reduce risk of hypoglycemia
        Inform patients using concomitant medications of risk of hypoglycemia and educate them on signs and symptoms of hypoglycemia
        Oral drugs with narrow therapeutic index
        Caution/dosage modification
        Tirzepatide may delay gastric emptying, thereby potentially impacting oral absorption
        Caution with drugs having a narrow therapeutic index (eg, warfarin)
        Advise patients using oral hormonal contraceptives to switch to a non-oral contraceptive method, or to add a barrier method of contraception for 4 weeks after initiation and for 4 weeks after each tirzepatide dose escalation

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