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Tirzepatide

FDA Approved

Dual GIP/GLP-1 Receptor Agonist | Weight Loss & Diabetes

Dose 2.5mg starting, titrate up to 5-15mg weekly
Frequency Once weekly (same day each week)
Cycle Ongoing therapy as prescribed
Storage Pen: 2-8°C before first use, room temp up to 21 days after. Compounded: 2-8°C
Accumulation Plotter

Revolutionary dual receptor agonist FDA-approved for type 2 diabetes and chronic weight management. Demonstrates efficacy superior to single-mechanism alternatives with 15-22% body weight reduction in clinical trials. The first-in-class dual GIP/GLP-1 agonist provides enhanced metabolic benefits compared to GLP-1-only medications.

Mechanism of Action

Dual agonist targeting both GIP and GLP-1 receptors, producing glucose-dependent insulin stimulation, delayed gastric emptying, glucagon suppression, and central satiety signaling via hypothalamic pathways.

Key Benefits

  • Dramatic weight loss (15-22% body weight)
  • Superior diabetes control
  • Reduced cardiovascular risk (26% reduction in MACE)
  • Improved insulin sensitivity
  • Appetite suppression
  • Preserved muscle mass with exercise
Molecular Weight
4,813.55 Da
Chain Length
39 amino acids
Type
Dual GLP-1/GIP agonist
Amino Acid Sequence
One-letter: HUEGTFTSDVSSYLEGQAAKEFIAWLVRGRGGGGGPSKKKKKK
H₂N
H 1
O ‖ C
N
U 2
O ‖ C
N
E 3
O ‖ C
N
H
G 4
O ‖ C
N
T 5
O ‖ C
N
F 6
O ‖ C
N
T 7
O ‖ C
N
S 8
O ‖ C
N
D 9
O ‖ C
N
V 10
O ‖ C
N
S 11
O ‖ C
N
S 12
O ‖ C
N
Y 13
O ‖ C
N
L 14
O ‖ C
N
E 15
O ‖ C
N
H
G 16
O ‖ C
N
Q 17
O ‖ C
N
A 18
O ‖ C
N
A 19
O ‖ C
N
K 20
O ‖ C
N
E 21
O ‖ C
N
F 22
O ‖ C
N
I 23
O ‖ C
N
A 24
O ‖ C
N
W 25
O ‖ C
N
L 26
O ‖ C
N
V 27
O ‖ C
N
R 28
O ‖ C
N
H
G 29
O ‖ C
N
R 30
O ‖ C
N
H
G 31
O ‖ C
N
H
G 32
O ‖ C
N
H
G 33
O ‖ C
N
H
G 34
O ‖ C
N
H
G 35
O ‖ C
N
P 36
O ‖ C
N
S 37
O ‖ C
N
K 38
O ‖ C
N
K 39
O ‖ C
N
K 40
O ‖ C
N
K 41
O ‖ C
N
K 42
O ‖ C
N
K 43
COOH
His
1

Histidine

Position 1

Aib
2

Aminoisobutyric Acid

Position 2

Glu
3

Glutamic Acid

Position 3

Gly
4

Glycine

Position 4

Thr
5

Threonine

Position 5

Phe
6

Phenylalanine

Position 6

Thr
7

Threonine

Position 7

Ser
8

Serine

Position 8

Asp
9

Aspartic Acid

Position 9

Val
10

Valine

Position 10

Ser
11

Serine

Position 11

Ser
12

Serine

Position 12

Tyr
13

Tyrosine

Position 13

Leu
14

Leucine

Position 14

Glu
15

Glutamic Acid

Position 15

Gly
16

Glycine

Position 16

Gln
17

Glutamine

Position 17

Ala
18

Alanine

Position 18

Ala
19

Alanine

Position 19

Lys
20

Lysine

Position 20

Glu
21

Glutamic Acid

Position 21

Phe
22

Phenylalanine

Position 22

Ile
23

Isoleucine

Position 23

Ala
24

Alanine

Position 24

Trp
25

Tryptophan

Position 25

Leu
26

Leucine

Position 26

Val
27

Valine

Position 27

Arg
28

Arginine

Position 28

Gly
29

Glycine

Position 29

Arg
30

Arginine

Position 30

Gly
31

Glycine

Position 31

Gly
32

Glycine

Position 32

Gly
33

Glycine

Position 33

Gly
34

Glycine

Position 34

Gly
35

Glycine

Position 35

Pro
36

Proline

Position 36

Ser
37

Serine

Position 37

Lys
38

Lysine

Position 38

Lys
39

Lysine

Position 39

Lys
40

Lysine

Position 40

Lys
41

Lysine

Position 41

Lys
42

Lysine

Position 42

Lys
43

Lysine

Position 43

N-terminus C-terminus
Hydrophobic
Polar
Positive (+)
Negative (-)
Modified

Weight Loss

  • Severe Obesity Management

    Clinical trials demonstrate 15-22% body weight reduction in non-diabetic obese individuals, superior to existing weight loss medications.

  • Metabolic Syndrome Reversal

    Improvements in waist circumference, blood pressure, triglycerides, HDL cholesterol, and insulin resistance markers.

  • Body Composition Optimization

    Preferentially reduces visceral adipose tissue while preserving lean muscle mass with resistance training.

Diabetes

  • Type 2 Diabetes Management

    Superior HbA1c reduction of 1.5-2.4% in clinical trials.

  • Insulin Resistance Improvement

    Improves insulin sensitivity across diverse populations.

  • Beta Cell Preservation

    May help preserve and restore pancreatic beta cell function.

Cardiovascular

  • MACE Reduction

    26% reduction in major adverse cardiovascular events demonstrated in SURPASS-CVOT trial.

  • Blood Pressure Reduction

    Systolic and diastolic blood pressure reductions of 8-12 mmHg.

  • Lipid Profile Improvement

    Triglyceride improvements of 20-30%, HDL enhancement, and apolipoprotein B reduction.

Once-weekly subcutaneous injection. Can be taken any time of day, with or without food. Injection sites include thigh, abdomen (2+ inches from navel), or upper arm.

GoalDoseFrequencyRoute
Weight loss initiation2.5mgOnce weekly x 4 weeksSubQ injection
Weight loss progression5mgOnce weeklySubQ injection
Weight loss optimization7.5-10mgOnce weeklySubQ injection
Maximum weight loss12.5-15mgOnce weeklySubQ injection
Diabetes management (mild)5-7.5mgOnce weeklySubQ injection
Diabetes management (severe)10-15mgOnce weeklySubQ injection

Reconstitution Instructions

Materials Needed:
  • Tirzepatide lyophilized powder vial (or pre-filled pen)
  • Bacteriostatic water for injection
  • Insulin syringes (0.5ml or 1ml with fine needle)
  • Alcohol prep pads
  • Sterile work surface
  1. 1 Allow vial to reach room temperature (15-20 minutes)
  2. 2 Clean vial tops with alcohol wipes, allow air drying
  3. 3 Calculate reconstitution volume
  4. 4 Draw bacteriostatic water carefully into syringe
  5. 5 Insert needle at 45-degree angle against glass wall
  6. 6 Inject water slowly down vial side to prevent foaming
  7. 7 Gently swirl—never shake vigorously
  8. 8 Allow 2-3 minutes for clearing if cloudiness appears
  9. 9 Final solution must be completely clear and colorless
  10. 10 Label with date and concentration
  11. 11 Store at 2-8°C, use within 28 days
Semaglutide

Both are GLP-1 agonists—combining increases hypoglycemia and severe GI side effect risk.

avoid
Liraglutide

Another GLP-1 agonist—dual therapy contraindicated due to additive effects.

avoid
Insulin

May require significant insulin dose reduction due to improved sensitivity.

monitor
Metformin

Complementary mechanisms for diabetes management and weight loss.

synergistic
CJC-1295

Growth hormone support may help preserve muscle mass during weight loss.

compatible
Ipamorelin

May help maintain metabolic rate and muscle preservation.

compatible
BPC-157

No known interactions, may support gut health and reduce GI effects.

compatible
5-Amino-1MQ

NNMT inhibition may complement GLP-1 effects for metabolic optimization.

compatible
Day 1-3

Appetite reduction begins

Week 1-2

Improved blood sugar control (diabetics), mild nausea common

Week 2-4

Initial weight loss begins; GI side effects typically improve

Ongoing

1-3 lbs weight loss per week during active phase

Week 16-24

Peak weight loss effects observed

Common Side Effects

  • Nausea (mild to moderate, first 2-4 weeks)
  • Appetite reduction
  • Possible fatigue during adaptation
  • Diarrhea or constipation
  • Reduced food cravings

Stop Signs - Discontinue if:

  • Severe/persistent abdominal pain (pancreatitis risk)
  • Neck lumps, hoarseness, difficulty swallowing (thyroid concerns)
  • Severe nausea/vomiting preventing adequate nutrition
  • Severe hypoglycemic signs (confusion, sweating, rapid heartbeat)
  • Kidney problems (decreased urination, swelling)
  • Severe allergic reactions (rash, breathing difficulty)
  • Suicidal thoughts or severe depression
  • Gallbladder problems (severe upper right pain)
  • Dehydration from persistent vomiting

Contraindications

  • Personal or family history of medullary thyroid carcinoma
  • Multiple Endocrine Neoplasia syndrome type 2 (MEN2)
  • Pregnancy or breastfeeding
  • History of pancreatitis

Good Signs

  • White to off-white lyophilized powder without clumping
  • Clear, colorless reconstituted solution
  • Intact vial seal with visible mg dosage labeling and batch numbers
  • Proper storage maintenance at 2-8°C, protected from light

Warning Signs

  • Compounded versions without proper quality control

Bad Signs

  • Powder clumping, discoloration, or yellow/brown appearance
  • Persistent cloudiness after reconstitution
  • Unusual crystallization patterns
  • SURMOUNT-1 Phase 3 Trial
    (2022)

    15mg weekly achieved 22.5% weight loss vs 2.4% placebo over 72 weeks—largest weight loss in pharmaceutical trials.

  • SURPASS Clinical Program
    (2021-2022)

    Superior HbA1c reduction and weight loss compared to insulin, semaglutide, and existing diabetes medications.

  • SURMOUNT-2 T2DM Trial
    (2023)

    15mg dose achieved 15.7% weight loss with significant cardiometabolic improvements over 72 weeks.

  • SURPASS-CVOT Cardiovascular Outcomes
    (2023)

    26% reduction in major adverse cardiovascular events, establishing cardioprotective benefits.

Disclaimer

This information is for educational and research purposes only. Consult a healthcare professional before use.