Tirzepatide - Drug Information
Tirzepatide - Drug Information
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Contributor Disclosures
Special Alerts
The FDA has been evaluating reports of suicidal thoughts or actions in patients
treated with glucagon-like peptide-1 receptor agonists (GLP-1 RAs). A
preliminary evaluation has not found evidence that the use of these medicines
causes suicidal thoughts or actions, but the FDA is continuing to investigate this
issue. Patients should not stop taking GLP-1 RAs without consulting their health
care provider. Health care providers should monitor for and advise patients
using GLP-1 RAs to report new or worsening depression, suicidal thoughts, or
any unusual changes in mood or behavior.
In both male and female rats, tirzepatide causes dose-dependent and treatment-
duration-dependent thyroid C-cell tumors at clinically relevant exposures. It is
unknown whether tirzepatide causes thyroid C-cell tumors, including medullary
thyroid carcinoma (MTC), in humans as human relevance of tirzepatide-induced
rodent thyroid C-cell tumors has not been determined.
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inform them of symptoms of thyroid tumors (eg, a mass in the neck, dysphagia,
dyspnea, persistent hoarseness). Routine monitoring of serum calcitonin or
using thyroid ultrasound is of uncertain value for early detection of MTC in
patients treated with tirzepatide.
Brand Names: US
Mounjaro; Zepbound
Pharmacologic Category
Glucose-Dependent Insulinotropic Polypeptide (GIP)/Glucagon-Like Peptide (GLP-1)
Receptor Agonist
Dosing: Adult
Dosage guidance:
Missed doses:
Single missed dose: Administer missed dose as soon as possible within 4 days, then
resume usual schedule thereafter. If >4 days have elapsed, skip the missed dose
and resume administration at the next scheduled weekly dose.
Multiple missed doses: For patients on the 2.5 mg/week dose, reinitiate at 2.5 mg once
weekly. For patients on doses ≥5 mg/week:
If 2 or fewer doses missed: Reinitiate at the same dose if previously tolerated (Ref).
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Adverse Reactions
The following adverse drug reactions and incidences are derived from product labeling
unless otherwise specified. Adverse reactions reported in adults.
>10%:
1% to 10%:
<1%:
Gastrointestinal: Dysgeusia
Postmarketing:
Contraindications
Warnings/Precautions
Disease-related concerns:
• Bariatric surgery:
• Delayed gastric emptying: Tirzepatide slows gastric emptying, which may alter the
absorption of other medications. Monitor narrow therapeutic index medications
for increased or decreased response.
Other warnings/precautions:
• Appropriate use: Diabetes mellitus: Do not use in patients with type 1 diabetes
mellitus or for the treatment of diabetic ketoacidosis; not a substitute for insulin.
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risks and benefits of this approach have not been evaluated (AGA [Hashash 2023];
ASA [Joshi 2023]). For example, in patients using GLP-1 RAs for glycemic control,
holding the medication may result in perioperative hyperglycemia and increase
the risk of adverse postoperative outcomes (AGA [Hashash 2023]; van Zuylen
2024). Individualize the decision to hold the GLP-1 RA based on patient-specific
factors such as the indication (eg, glycemic control vs weight management),
duration and frequency of therapy, presence of adverse GI symptoms, and
concomitant medications that may slow gastric emptying (eg, opioids, proton
pump inhibitors); may consider additional preoperative interventions (eg, clear
liquid diet, full stomach precautions, gastric ultrasound) on a case-by-case basis to
reduce risk (ASA [Hashash 2023]; Marroquin-Harris 2023; Raven 2024; van Zuylen
2024). Refer also to institutional protocols.
Dosage Forms: US
Excipient information presented when available (limited, particularly for generics); consult
specific product labeling.
Zepbound: 2.5 mg/0.5 mL (0.5 mL); 5 mg/0.5 mL (0.5 mL); 7.5 mg/0.5 mL (0.5 mL); 10
mg/0.5 mL (0.5 mL); 12.5 mg/0.5 mL (0.5 mL); 15 mg/0.5 mL (0.5 mL)
Mounjaro: 2.5 mg/0.5 mL (0.5 mL); 5 mg/0.5 mL (0.5 mL); 7.5 mg/0.5 mL (0.5 mL); 10
mg/0.5 mL (0.5 mL); 12.5 mg/0.5 mL (0.5 mL); 15 mg/0.5 mL (0.5 mL)
Zepbound: 2.5 mg/0.5 mL (0.5 mL); 5 mg/0.5 mL (0.5 mL); 7.5 mg/0.5 mL (0.5 mL); 10
mg/0.5 mL (0.5 mL); 12.5 mg/0.5 mL (0.5 mL); 15 mg/0.5 mL (0.5 mL)
Pricing: US
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Solution, Subcutaneous:
Mounjaro: 2.5 mg/0.5 mL (0.5 mL); 5 mg/0.5 mL (0.5 mL); 7.5 mg/0.5 mL (0.5 mL); 10
mg/0.5 mL (0.5 mL); 12.5 mg/0.5 mL (0.5 mL); 15 mg/0.5 mL (0.5 mL)
Mounjaro: 2.5 mg/0.5 mL (0.5 mL); 5 mg/0.5 mL (0.5 mL); 7.5 mg/0.5 mL (0.5 mL); 10
mg/0.5 mL (0.5 mL); 12.5 mg/0.5 mL (0.5 mL); 15 mg/0.5 mL (0.5 mL)
Mounjaro KwikPen: 2.5 mg/0.6 mL (2.4 mL); 5 mg/0.6 mL (2.4 mL); 7.5 mg/0.6 mL (2.4
mL); 10 mg/0.6 mL (2.4 mL); 12.5 mg/0.6 mL (2.4 mL); 15 mg/0.6 mL (2.4 mL)
[contains benzyl alcohol, phenol]
Zepbound KwikPen: 2.5 mg/0.6 mL (2.4 mL); 5 mg/0.6 mL (2.4 mL); 7.5 mg/0.6 mL (2.4
mL); 10 mg/0.6 mL (2.4 mL); 12.5 mg/0.6 mL (2.4 mL); 15 mg/0.6 mL (2.4 mL)
[contains benzyl alcohol, phenol]
Administration: Adult
SUBQ: Administer by SUBQ injection into the abdomen, thigh, or upper arm at any time of
day on the same day each week, with or without food. If changing the day of
administration is necessary, allow ≥72 hours between 2 doses. Rotate injection sites
with each dose. When using the single-dose vial use a syringe appropriate for dose
administration (eg, a 1 mL syringe for measuring a 0.5 mL dose). Do not mix with other
injectable products (eg, insulin); administer as separate injections. Avoid adjacent
injections if administering other agents in the same area of the body. Solution should
be clear and colorless to slightly yellow; do not use if particulate matter or
discoloration are seen. Do not inject into skin that has lumps or pits or skin that is
bruised, damaged, hard, scaly, scarred, tender, or thickened.
Mounjaro and Zepbound single-dose pens do not require priming before injection. For the
Mounjaro Kwikpen and Zepbound Kwikpen multidose pens (Canadian products), prime
the needle before injecting by turning the dose selector 2 clicks to the prime indicator
and injecting into the air. Use a new needle for each injection. Once injected into the
body, continue to depress the button until the dial has returned to 0 and for an
additional 5 seconds. Then, remove the needle.
An FDA-approved patient medication guide, which is available with the product information
and as follows, must be dispensed with this medication:
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Mounjaro:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/215866s002s006lb
l.pdf#page=20
Limitations of use: Has not been studied in patients with a history of pancreatitis; not
indicated for use in patients with type 1 diabetes mellitus.
Heart failure with preserved ejection fraction, weight management; Metabolic dysfunction–
associated steatohepatitis, weight management
Sound-alike/look-alike issues:
Metabolism/Transport Effects
None known.
Drug Interactions
(For additional information: Launch drug interactions program)
Note: Interacting drugs may not be individually listed below if they are part of a group
interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a
complete list of drug interactions by individual drug name and detailed management
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recommendations, use the drug interactions program by clicking on the “Launch drug
interactions program” link above.
Alpha-Lipoic Acid: May increase hypoglycemic effects of Antidiabetic Agents. Risk C: Monitor
Androgens: May increase hypoglycemic effects of Agents with Blood Glucose Lowering
Effects. Risk C: Monitor
Direct Acting Antiviral Agents (HCV): May increase hypoglycemic effects of Antidiabetic
Agents. Risk C: Monitor
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Maitake: May increase hypoglycemic effects of Agents with Blood Glucose Lowering Effects.
Risk C: Monitor
Monoamine Oxidase Inhibitors: May increase hypoglycemic effects of Agents with Blood
Glucose Lowering Effects. Risk C: Monitor
Pegvisomant: May increase hypoglycemic effects of Agents with Blood Glucose Lowering
Effects. Risk C: Monitor
Prothionamide: May increase hypoglycemic effects of Agents with Blood Glucose Lowering
Effects. Risk C: Monitor
Quinolones: May increase hypoglycemic effects of Agents with Blood Glucose Lowering
Effects. Quinolones may decrease therapeutic effects of Agents with Blood Glucose
Lowering Effects. Specifically, if an agent is being used to treat diabetes, loss of blood
sugar control may occur with quinolone use. Risk C: Monitor
Salicylates: May increase hypoglycemic effects of Agents with Blood Glucose Lowering
Effects. Risk C: Monitor
Selective Serotonin Reuptake Inhibitor: May increase hypoglycemic effects of Agents with
Blood Glucose Lowering Effects. Risk C: Monitor
Sincalide: Drugs that Affect Gallbladder Function may decrease therapeutic effects of
Sincalide. Management: Consider discontinuing drugs that may affect gallbladder
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Reproductive Considerations
Agents other than tirzepatide are currently recommended for patients with type 2 diabetes
mellitus planning to become pregnant (ADA 2025).
Obesity increases the risk of infertility. Optimal weight control prior to conception improves
pregnancy outcomes; however, medications for weight loss are not recommended prior to
pregnancy due to safety issues and adverse events. Weight loss medications should be
discontinued prior to conception (ACOG 2021; Wharton 2020).
Tirzepatide may decrease the efficacy of oral hormonal contraception due to changes in
gastric emptying; contraceptives administered by a nonoral route are not affected. Because
the changes in gastric emptying are largest following the first dose, patients using an oral
contraceptive should add a barrier method for 4 weeks after starting tirzepatide treatment
and for 4 weeks after each dose increase. Alternately, patients can be switched to nonoral
contraceptive methods.
Consult drug interactions database for more detailed information specific to use of
tirzepatide and specific contraceptives.
Pregnancy Considerations
Based on data from animal reproduction studies, in utero exposure to tirzepatide may
cause fetal harm.
Poorly controlled diabetes during pregnancy can be associated with an increased risk of
adverse maternal and fetal outcomes, including diabetic ketoacidosis, preeclampsia,
spontaneous abortion, preterm delivery, delivery complications, major malformations,
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stillbirth, and macrosomia (ACOG 2018). To prevent adverse outcomes, prior to conception
and throughout pregnancy, maternal blood glucose and HbA1c should be kept as close to
target goals as possible but without causing significant hypoglycemia (ADA 2025).
Agents other than tirzepatide are currently recommended to treat diabetes mellitus in
pregnancy (ADA 2025).
An increased risk of adverse maternal and fetal events is associated with obesity; however,
moderate gestational weight gain based on prepregnancy BMI is required for positive fetal
outcomes in all pregnancies, including patients who are overweight or obese. Therefore,
medications for weight loss therapy are not recommended during pregnancy (ACOG 2021;
Wharton 2020). Patients should discontinue tirzepatide once pregnancy is recognized.
Breastfeeding Considerations
According to the manufacturer, the decision to breastfeed during therapy should consider
the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits
of treatment to the mother.
Monitoring Parameters
Plasma glucose; GI adverse reactions (eg, nausea, vomiting, diarrhea); kidney function (at
baseline and following dose increases in patients with kidney impairment reporting
severe GI adverse reactions); signs/symptoms of pancreatitis (eg, persistent severe
abdominal pain, which may radiate to the back and that may or may not be
accompanied by vomiting); signs/symptoms of gallbladder disease; worsening of
diabetic retinopathy (particularly in those with a prior history of the disease);
emergence of worsening depression, suicidal thoughts/behavior, changes in behavior;
heart rate; body weight (when used for chronic weight management).
HbA1c: Monitor at least 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. Note: In patients prone to
glycemic variability (eg, patients with insulin deficiency), or in patients whose
HbA1c is discordant with serum glucose levels or symptoms, consider evaluating
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Reference Range
HbA1c: <7% (a more aggressive [<6.5%] or less aggressive [<8%] HbA1c goal may be
targeted based on patient-specific characteristics). Note: In patients using a
continuous glucose monitoring system, a goal of time in range >70% with time
below range <4% is recommended and is similar to a goal HbA1c <7%.
Preprandial capillary blood glucose: 80 to 130 mg/dL (SI: 4.4 to 7.2 mmol/L) (more
or less stringent goals may be appropriate based on patient-specific
characteristics).
Peak postprandial capillary blood glucose (~1 to 2 hours after a meal): <180 mg/dL
(SI: <10 mmol/L) (more or less stringent goals may be appropriate based on
patient-specific characteristics).
Note: Consider less strict targets in patients who are using insulin and/or insulin
secretagogues (sulfonylureas, meglitinides) (ES [LeRoith 2019]).
Preprandial capillary blood glucose: 80 to 130 mg/dL (SI: 4.4 to 7.2 mmol/L)
(healthy); 90 to 150 mg/dL (SI: 5 to 8.3 mmol/L) (complex/intermediate health);
100 to 180 mg/dL (SI: 5.6 to 10 mmol/L) (very complex/poor health).
Bedtime capillary blood glucose: 80 to 180 mg/dL (SI: 4.4 to 10 mmol/L) (healthy);
100 to 180 mg/dL (SI: 5.6 to 10 mmol/L) (complex/intermediate health); 110 to
200 mg/dL (SI: 6.1 to 11.1 mmol/L) (very complex/poor health).
Level 1: 54 to 70 mg/dL (SI: 3 to 3.9 mmol/L); hypoglycemia alert value; initiate fast-
acting carbohydrate (eg, glucose) treatment.
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Level 2: <54 mg/dL (SI: <3 mmol/L); threshold for neuroglycopenic symptoms; requires
immediate action.
Mechanism of Action
Tirzepatide is a glucose-dependent insulinotropic polypeptide (GIP) receptor and glucagon-
like peptide-1 (GLP-1) receptor agonist that increases glucose-dependent insulin secretion,
decreases inappropriate glucagon secretion, slows gastric emptying, and decreases food
intake (likely due to appetite mediation).
Bioavailability: 80%.
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