HUMALOG PEN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for HUMALOG PEN (HUMALOG PEN).

How it works

Insulin lispro is a rapid-acting insulin analog that binds to the insulin receptor, activating tyrosine kinase activity and downstream signaling pathways (e.g., PI3K/Akt) to promote glucose uptake in skeletal muscle and adipose tissue, inhibit hepatic gluconeogenesis, and regulate lipid and protein metabolism.

What the body does with it

Metabolism	Insulin lispro is metabolized primarily by insulin-degrading enzyme (IDE) and possibly other proteases; the exact pathways are not fully characterized. No significant CYP450 metabolism.
Excretion	Renal: 60-80% of dose excreted as metabolites; remainder hepatobiliary and fecal.
Half-life	Approximately 0.5-1 hour (rapid; subcutaneous absorption rate-limited).
Protein binding	<10% bound to plasma proteins (mainly albumin).
Volume of Distribution	0.26-0.36 L/kg (approximates extracellular fluid volume).
Bioavailability	Subcutaneous: 55-75% (due to local degradation at injection site).
Onset of Action	Subcutaneous: 10-20 minutes.
Duration of Action	Subcutaneous: 3-5 hours (short-acting; dose-dependent).

Classification & Brands

Dosing & administration

Subcutaneously 0.5–1 unit/kg/day divided into multiple doses (usually 3 or more), administered 15 minutes before or immediately after meals.

Dosage form	INJECTABLE
Renal impairment	No specific dose adjustment guidelines for renal impairment; however, reduced insulin requirements may occur with severe renal impairment (GFR <30 mL/min). Monitor glucose closely and titrate doses accordingly.
Liver impairment	No specific adjustment based on Child-Pugh score; hepatic impairment may reduce gluconeogenesis and increase insulin sensitivity, necessitating dose reduction. Monitor glucose and adjust cautiously.
Pediatric use	Children: 0.5–1 unit/kg/day subcutaneously divided into multiple doses (e.g., 3 or more). For type 1 diabetes, typical total daily dose is 0.5–1 unit/kg; adjust based on glycemic response.
Geriatric use	Elderly: Lower initial doses (e.g., 0.2–0.4 unit/kg/day) due to increased risk of hypoglycemia, with careful titration based on glucose monitoring. Impaired renal function may further reduce requirements.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for HUMALOG PEN (HUMALOG PEN).

Breastfeeding	Insulin lispro is a large protein molecule that is not expected to pass into breast milk in clinically significant amounts. No specific M/P ratio reported. Exogenous insulin is not orally bioavailable to the infant. Compatible with breastfeeding.
Teratogenic Risk	Insulin lispro does not cross the placenta in significant amounts. No increased risk of major congenital anomalies or spontaneous abortion when used during pregnancy. Poorly controlled diabetes during pregnancy increases maternal and fetal risks, including congenital anomalies (1st trimester), macrosomia, and neonatal hypoglycemia (2nd/3rd trimester).

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to insulin lispro or any of its excipients; during episodes of hypoglycemia

Clinical Precautions

Precautions

Hypoglycemia is the most common adverse effect. Never mix with insulins of other concentrations. Changes in insulin strength, manufacturer, type, or method of administration may affect glycemic control and predispose to hypoglycemia or hyperglycemia. Monitor glucose closely during illness, emotional disturbances, or stress. Use caution in patients with renal or hepatic impairment. Hypokalemia may occur. Injection site reactions and lipodystrophy are possible.

Clinical Tips & Counseling

Drug interactions

Loading safety data…

HUMALOG PEN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for HUMALOG PEN (HUMALOG PEN).

How it works

What the body does with it

Metabolism	Insulin lispro is metabolized primarily by insulin-degrading enzyme (IDE) and possibly other proteases; the exact pathways are not fully characterized. No significant CYP450 metabolism.
Excretion	Renal: 60-80% of dose excreted as metabolites; remainder hepatobiliary and fecal.
Half-life	Approximately 0.5-1 hour (rapid; subcutaneous absorption rate-limited).
Protein binding	<10% bound to plasma proteins (mainly albumin).
Volume of Distribution	0.26-0.36 L/kg (approximates extracellular fluid volume).
Bioavailability	Subcutaneous: 55-75% (due to local degradation at injection site).
Onset of Action	Subcutaneous: 10-20 minutes.
Duration of Action	Subcutaneous: 3-5 hours (short-acting; dose-dependent).

Classification & Brands

Dosing & administration

Subcutaneously 0.5–1 unit/kg/day divided into multiple doses (usually 3 or more), administered 15 minutes before or immediately after meals.

Dosage form	INJECTABLE
Renal impairment	No specific dose adjustment guidelines for renal impairment; however, reduced insulin requirements may occur with severe renal impairment (GFR <30 mL/min). Monitor glucose closely and titrate doses accordingly.
Liver impairment	No specific adjustment based on Child-Pugh score; hepatic impairment may reduce gluconeogenesis and increase insulin sensitivity, necessitating dose reduction. Monitor glucose and adjust cautiously.
Pediatric use	Children: 0.5–1 unit/kg/day subcutaneously divided into multiple doses (e.g., 3 or more). For type 1 diabetes, typical total daily dose is 0.5–1 unit/kg; adjust based on glycemic response.
Geriatric use	Elderly: Lower initial doses (e.g., 0.2–0.4 unit/kg/day) due to increased risk of hypoglycemia, with careful titration based on glucose monitoring. Impaired renal function may further reduce requirements.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for HUMALOG PEN (HUMALOG PEN).

Breastfeeding	Insulin lispro is a large protein molecule that is not expected to pass into breast milk in clinically significant amounts. No specific M/P ratio reported. Exogenous insulin is not orally bioavailable to the infant. Compatible with breastfeeding.
Teratogenic Risk	Insulin lispro does not cross the placenta in significant amounts. No increased risk of major congenital anomalies or spontaneous abortion when used during pregnancy. Poorly controlled diabetes during pregnancy increases maternal and fetal risks, including congenital anomalies (1st trimester), macrosomia, and neonatal hypoglycemia (2nd/3rd trimester).

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

Hypersensitivity to insulin lispro or any of its excipients; during episodes of hypoglycemia