lamivudine/raltegravir

Action and Spectrum

Actions and Spectrum 

lamivudine is an NRTI (nucleoside reverse transcriptase inhibitor) drug class member. The reverse transcriptase enzyme, which is necessary for the reproduction of HIV, is mostly inhibited by it.   

A wide range of HIV-1 strains, including drug-resistant and wild-type strains, are responsive to lamivudine. The class of drugs known as integrase strand transfer inhibitors (INSTIs) includes raltegravir.

The integrase enzyme, which is responsible for integrating the viral DNA into the DNA of the host cell, is the target of its mechanism of action. raltegravir is effective against HIV-1 strains, including drug-resistant and wild-type viruses. 

Drug Interaction

Adverse Reaction

Frequency defined  

>10%  

For raltegravir 

Total cholesterol increased (16%) 

>10%  

For lamivudine  

Nausea  

Vomiting 

Pancreatitis 

Musculoskeletal pain 

Peripheral neuropathy 

Nervous system neuropathy 

Fever (pediatric) 

Headache 

Cough 

Fatigue and malaise 

Diarrhea 

1-10%  

For lamivudine 

Abdominal cramps, abdominal pain 

Dizziness  

Thrombocytopenia 

Insomnia 

Rash 

Arthralgia 

Creatine phosphokinase increased  

Myalgia 

Depression 

Chills 

Dyspepsia 

Anorexia and decreased appetite 

1-10%  

For raltegravir 

Abdominal pain (5%) 

Arthralgia (3%) 

Influenza (3%) 

Pyrexia 

Rash (5%)  

Dizziness (4%) 

Extremity pain (3%) 

Nausea 

Vomiting (4%) 

AST increased (9%) 

Nasopharyngitis (6%) 

Diarrhea 

Insomnia (4%) 

Glucose increased (9%) 

Cough (5%) 

Hyperbilirubinemia (9%) 

Fatigue (8%) 

<1%  

For raltegravir 

Thrombocytopenia 

Renal failure 

Drug related hypersensitivity 

Suicidal ideation 

Asthenia gastrointestinal disorders 

Skin disorders 

Lipodystrophy 

Frequency Not Defined  

For lamivudine  

Neutropenia 

Hepatitis B exacerbation 

Body fat redistribution 

Elevated amylase 

Post marketing Reports  

For raltegravir 

Diarrhea  

Thrombocytopenia  

Psychiatric disorders: including suicidal ideation and behaviors, paranoia, anxiety, depression 

Rhabdomyolysis 

Skin: Steven’s-Johnson syndrome, rash  

Cerebellar ataxia 

Hepatic failure 

Black Box Warning

Black Box Warning 

None

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• lamivudine/raltegravir is contraindicated in individuals with a known hypersensitivity or previous serious allergic reaction to lamivudine/raltegravir or any of its components. 

Caution: 

• Caution should be exercised when administering lamivudine/raltegravir to individuals with significant renal impairment. 
• lamivudine/raltegravir should be used with caution in individuals with hepatic impairment.  
• Occurrences of hepatitis aggravation after treatment were recorded in individuals who are co-infected with HIV-1 and hepatitis B virus. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: C 

Lactation: Excretion into human milk is unknown and lactation should be avoided   

Pregnancy Categories:         

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.  

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women. 

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 

Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology  

lamivudine is a nucleoside reverse transcriptase inhibitor. It inhibits the reverse transcriptase enzyme of HIV and hepatitis B virus. 

raltegravir is an integrase strand transfer inhibitor. It inhibits the integrase enzyme of HIV-1.  

Pharmacodynamics 

HIV-1 can be inhibited by lamivudine. Both wild-type strains and some strains with resistance mutations are susceptible to their effectiveness.   

raltegravir is effective against HIV-1 strains, including those strains with resistance mutations as well as wild-type strains. 

Pharmacokinetics 

Absorption   

lamivudine is well-absorbed after oral administration, with an oral bioavailability of around 80%.  

raltegravir is well-absorbed after oral administration, with an oral bioavailability of around 33%. 

Distribution 

lamivudine has a small volume of distribution; thus, it is distributed predominantly in the extracellular fluid. 

raltegravir has a moderate volume of distribution, hence distributes widely throughout the body. 

Metabolism 

lamivudine is not extensively metabolized. It undergoes minimal hepatic metabolism.  

raltegravir undergoes metabolism primarily via glucuronidation in the liver.  

Elimination and excretion 

Most of the lamivudine is eliminated by the kidneys via glomerular filtration. 

The majority of raltegravir and its metabolites are excreted in via biliary excretion.

Adminstartion

Administration 

lamivudine and raltegravir are both antiretroviral medications and they are mainly available in tablet form.  

It should be swallowed whole with water and can be taken with or without food.

Patient Information Leaflet

Patient information leaflet 

Generic Name: lamivudine/raltegravir  

Why do we use lamivudine/raltegravir? 

lamivudine/raltegravir are both medications used in the treatment of HIV infection.  

lamivudine/raltegravir is used as part of combination antiretroviral therapy (ART) for the treatment of HIV-1 infection in adults and children.  

lamivudine is also used for the treatment of chronic hepatitis B (HBV) infection in adults and children.   

raltegravir helps suppress viral replication, improve immune function, and delay the progression of HIV disease.