tirzepatide

tir-ZEP-a-tide

Therapeutic Classification: antidiabetics

Pharmacologic Classification: glucagon like peptide 1 glp 1 receptor agonists, glucose dependent insulinotropic polypeptide gip receptor agonists

REMS

Mounjaro

Type 2 diabetes mellitus (as adjunct to diet and exercise).

Zepbound

Treatment of the following conditions:
- Chronic weight management in patients who are obese (body mass index [BMI] ≥30 kg/m²) OR are overweight (BMI ≥27 kg/m²) with ≥1 weight-related comorbid condition (e.g., hypertension, dyslipidemia, type 2 diabetes, obstructive sleep apnea, or cardiovascular disease) (in combination with reduced-calorie diet and increased physical activity).
- Moderate to severe obstructive sleep apnea in patients with obesity.

Acts as a glucose-dependent insulinotropic polypeptide receptor and glucagon-like peptide-1 (GLP-1) receptor agonist; increases insulin secretion and reduces glucagon secretion, both in a glucose-dependent manner. Also slows gastric emptying. Also helps to suppress appetite, leading to decreased caloric intake.

Therapeutic effects:

Improved glycemic control.
Reduction in body weight.
Reduction in apneic/hypoapneic episodes per hour.

Absorption: 80% absorbed following subcutaneous administration.

Distribution: Minimally distributed to tissues.

Protein Binding: 99%.

Metabolism/Excretion: Metabolized by proteolytic cleavage, beta oxidation, and amide hydrolysis. Excreted in the urine and feces, with very little being eliminated as unchanged drug.

Half-Life: 5 days.

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
SUBQ	unknown	8–72 hr	unknown

Contraindicated in:

Hypersensitivity;
Personal or family history of medullary thyroid carcinoma
;
Multiple endocrine neoplasia syndrome type 2
;
Type 1 diabetes;
Severe GI disease (including severe gastroparesis).

Use Cautiously in:

History of pancreatitis;
Diabetic retinopathy (↑ risk of complications);
History of angioedema or anaphylaxis to another GLP-1 receptor agonist;
History of suicide or active suicidal ideation;
Undergoing elective surgery or procedure requiring general anesthesia or deep sedation;
Rep: Women of reproductive potential;
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk; insulin recommended for glucose management in pregnancy;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children.

CV: ↑HR, hypotension

Derm: hair loss

EENT: retinopathy complications

Endo: hypoglycemia, MEDULLARY THYROID CARCINOMA

GI: ↓appetite, constipation, diarrhea, nausea, vomiting, ↑amylase, ↑lipase, abdominal distension, abdominal pain, cholecystitis, cholelithiasis, dyspepsia, flatulence, gastroesophageal reflux disease, PANCREATITIS

GU: acute kidney injury

Local: injection site reactions

Neuro: dizziness, dysesthesia, dysgeusia, fatigue, SUICIDAL THOUGHTS/BEHAVIOR

Resp: aspiration

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Drug-drug:

Concurrent use with agents that increase insulin secretion, including sulfonylureas or insulin, may ↑ the risk of serious hypoglycemia; use cautiously and consider dose ↓ of agent increasing insulin secretion.
May alter absorption of concurrently administered oral medications, including oral hormonal contraceptives, due to delayed gastric emptying; advise patients taking oral hormonal contraceptive to switch to a nonoral contraceptive method or add a barrier contraceptive method for 4 wk after initiating therapy and for 4 wk after each dose escalation of tirzepatide.

Type 2 Diabetes

SC (Adults ): Mounjaro: 2.5 mg once weekly initially for 4 wk; then ↑ to 5 mg once weekly; may then ↑ dose in 2.5 mg/wk increments every 4 wk, if needed, to achieve glycemic goals (max weekly dose = 15 mg/wk).

Chronic Weight Management

SC (Adults ): Zepbound: 2.5 mg once weekly initially for 4 wk; then ↑ to 5 mg once weekly; may then ↑ dose in 2.5 mg/wk increments every 4 wk, if needed, to achieve weight loss goals. Recommended maintenance dose is 5 mg/wk, 10 mg/wk, or 15 mg/wk.

Obstructive Sleep Apnea

SC (Adults ): Zepbound: 2.5 mg once weekly initially for 4 wk; then ↑ to 5 mg once weekly; then ↑ dose in 2.5 mg/wk increments every 4 wk to achieve recommended maintenance dose of 10 mg/wk or 15 mg/wk.

Solution for injection (prefilled pens and single-dose vials): 2.5 mg/0.5 mL; 5 mg/0.5 mL; 7.5 mg/0.5 mL; 10 mg/0.5 mL; 12.5 mg/0.5 mL; 15 mg/0.5 mL

Observe patient taking concurrent insulin for signs/symptoms of hypoglycemic reactions (sweating, hunger, weakness, dizziness, tremor, tachycardia, anxiety, headache, blurred vision, slurred speech, irritability).
If thyroid nodules or ↑ serum calcitonin are noted, patient should be referred to an endocrinologist.
Monitor for signs/symptoms of pancreatitis (persistent severe abdominal pain, sometimes radiating to the back, with or without vomiting). If pancreatitis suspected, discontinue tirzepatide. If pancreatitis confirmed, do not restart tirzepatide.
Monitor for signs/symptoms of hypersensitivity reactions (anaphylaxis, angioedema) during therapy.
Monitor for new or worsening depression, suicidal thoughts or behaviors, or any unusual changes in mood or behavior. If patient experiences suicidal thoughts or behaviors, discontinue tirzepatide.
Monitor weight before and periodically during therapy.

Lab Test Considerations:

Monitor A1c twice yearly in patients who have stable glycemic control and are meeting treatment goals. Monitor quarterly in patients in whom treatment goals have not been met or with therapy change.
- Zepbound: In patients with type 2 diabetes, monitor blood glucose prior to starting and during therapy.
- May ↑ lipase and amylase.

Patients stabilized on a diabetic regimen who are exposed to stress, fever, trauma, infection, or surgery may require administration of insulin.
SC: Administer once weekly at any time of the day, without regard to food. Day of week may be changed as long as ≥72 hr before next dose. The pen is a single-dose device that does not require priming before injection. Inject into abdomen, thigh, or upper arm. Rotate injection sites with each dose. Solution is clear and colorless to slightly yellow; do not administer solutions that are cloudy, discolored, or contain particulate matter. Store pens in refrigerator; can also be stored at room temperature for up to 21 days; do not freeze. Store in the original carton to protect from light.
When using with insulin, administer as separate injections; never mix. If injecting tirzepatide and insulin in same body region, injections should not be close to each other.

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Instruct patient on use of pen and to use as directed. Advise patient to rotate injection sites with each dose. Follow manufacturer's instructions for pen use. Pen should never be shared between patients, even if needle is changed. Store pen in refrigerator; do not freeze. After initial use, pen may be stored at room temperature for up to 21 days. Emphasize the importance of routine follow-up exams.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care provider before taking any new medications.
Take missed dose as soon as remembered within 4 days after the missed dose. If >4 days have passed, skip the missed dose and administer the next dose on the regularly scheduled day.
Advise patient taking insulin and tirzepatide to never mix insulin and tirzepatide together. Give as 2 separate injections. Both injections may be given in the same body area, but should not be given right next to each other.
Explain to patient that this medication controls hyperglycemia but does not cure diabetes. Therapy is long term.
Review signs/symptoms of hypoglycemia and hyperglycemia with patient. If hypoglycemia occurs, advise patient to take a glass of orange juice or 2–3 teaspoons of sugar, honey, or corn syrup dissolved in water and notify health care provider.
Encourage patient to follow prescribed diet, medication, and exercise regimen to prevent hypoglycemic or hyperglycemic episodes.
Instruct patient in proper testing of serum glucose and ketones. These tests should be closely monitored during periods of stress or illness, and health care provider should be notified if significant changes occur.
Advise patient to notify health care provider if changes in vision occur during therapy.
Advise patient to notify health care provider immediately if signs/symptoms of pancreatitis (nausea, vomiting, abdominal pain) or hypersensitivity (swelling of face, lips, tongue, or throat; problems breathing or swallowing; severe rash or itching; fainting or feeling dizzy; very rapid heartbeat) occur.
Inform patient of risk of benign and malignant thyroid tumors. Advise patient to notify health care provider if signs/symptoms of thyroid tumors (lump in neck, hoarseness, trouble swallowing, shortness of breath) occur.
Advise patient to inform health care provider of medication regimen before procedures or surgery due to ↑ risk of aspiration with general or deep sedation.
Advise patient to carry a form of sugar (sugar packets, candy) and identification describing disease process and medication regimen at all times.
Rep: Insulin is the preferred method of controlling blood glucose during pregnancy. Counsel women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding. Advise patients using oral hormonal contraceptives to switch to a nonoral contraceptive method or add a barrier method of contraception for 4 wk after initiation and for 4 wk after each dose escalation.

Improved glycemic control.
Reduction in body weight.
Reduction in apneic/hypoapneic episodes per hour.

Mounjaro, Zepbound

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Availability ⬆ ⬇

Assessment ⬆ ⬇

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆