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- Pharmacology For Lamivudine + Didanosine + Efavirenz
Lamivudine + Didanosine + Efavirenz Pharmacology
Lamivudine + Didanosine + EfavirenzAbout Lamivudine + Didanosine + EfavirenzN/AMechanism of Action of Lamivudine + Didanosine + EfavirenzN/APharmacokinets of Lamivudine + Didanosine + EfavirenzN/AOnset of Action for Lamivudine + Didanosine + EfavirenzN/ADuration of Action for Lamivudine + Didanosine + EfavirenzN/AHalf Life of Lamivudine + Didanosine + EfavirenzN/ASide Effects of Lamivudine + Didanosine + EfavirenzN/AContra-indications of Lamivudine + Didanosine + EfavirenzN/ASpecial Precautions while taking Lamivudine + Didanosine + EfavirenzN/APregnancy Related InformationN/AOld Age Related InformationN/ABreast Feeding Related InformationN/AChildren Related InformationN/AIndications for Lamivudine + Didanosine + EfavirenzN/AInteractions for Lamivudine + Didanosine + EfavirenzN/ATypical Dosage for Lamivudine + Didanosine + EfavirenzN/ASchedule of Lamivudine + Didanosine + EfavirenzN/AStorage Requirements for Lamivudine + Didanosine + EfavirenzN/AEffects of Missed Dosage of Lamivudine + Didanosine + EfavirenzN/AEffects of Overdose of Lamivudine + Didanosine + EfavirenzN/A
LamivudineAbout LamivudineNucleoside Reverse Transcriptase Inhibitor ,cytidine analogue, Antiretroviral.Mechanism of Action of LamivudineLamivudine is a deoxy cytidine nucleoside analogue. It undergoes phosphorylation in the presence of Kinase enzyme and form Lamivudine triphosphate. This Lamivudine triphosphate competitively inhibit HIV reverse transcriptase enzyme which is responsible for the conversion of viral RNA to pro viral DNA and is then added to host cell chromosome. Lamivudine triphosphate terminates elongation of pro viral DNA and results in inhibition of viral replication. Lamivudine triphosphate is also a potent inhibitor of HBV (hepatitis B virus)Pharmacokinets of LamivudineAbsorption: It is rapidly absorbed after oral administration. Distribution: It is widely distributed in the body. Metabolism: Metabolism is insignificant. Excretion: It is excreted in urineOnset of Action for LamivudineN/ADuration of Action for LamivudineN/AHalf Life of Lamivudine5 - 7 hoursSide Effects of Lamivudine1.Nausea
12.FeverContra-indications of LamivudineHypersensitivity to LamivudineSpecial Precautions while taking Lamivudine1.Renal impairment
2.Hepatic dysfunctionPregnancy Related InformationUse with cautionOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with caution
Indications for Lamivudine1.HIV infections
2.Treatment of chronic Hepatitis BInteractions for LamivudineTrimethoprim, sulfamethoxazole: Results in an increase in AUC of Lamivudine and a decrease in renal clearance.
Zidovudine: Results in an increase in C max. of Zidovudine.Typical Dosage for LamivudineAdult: 100 - 300 mg / day in 2 divided dose
HIV infection: 300 mg / day in 2 divided dose
Treatment of chronic Hepatitis B: 100 mg / day
Children: 4 - 8 mg / kg /day in 2 divided dose
HIV infection: 4 mg / kg /day in 2 divided dose
Schedule of LamivudineHStorage Requirements for LamivudineStore it at 15 -25 degree C in a tightly closed container .Protect away from heat and lightEffects of Missed Dosage of LamivudineTake the missed dose as soon as noticed and if it is the time to take the next dose then skip the missed dose and do not double the doseEffects of Overdose of LamivudineGive supportive measures and treatment.
DidanosineAbout DidanosineNucleoside Reverse Transcriptase Inhibitor, nucleoside analogue of adenosine, A systemic Antiretroviral agent.Mechanism of Action of DidanosineDidanosine is a deoxy adenosine nucleoside analogue. Intracellularly it undergoes phosphorylation in the presence of enzymes and finally forms active metabolite Dideoxy adenosine triphosphate. This Dideoxy adenosine triphosphate competitively inhibit HIV reverse transcriptase enzyme which is responsible for the conversion of viral RNA to pro viral DNA and is then added to host cell chromosome. Stavudine triphosphate terminates elongation of pro viral DNA and results in inhibition of viral replication.Pharmacokinets of DidanosineAbsorption: It is rapidly absorbed after oral administration. Distribution: It is widely distributed in the body .Metabolism: Metabolism is insignificant Excretion: It is excreted in urine.Onset of Action for Didanosine30 - 60 minuteDuration of Action for DidanosineN/AHalf Life of Didanosine90 minute; Dideoxy adenosine triphosphate: 25 - 40 hourSide Effects of Didanosine1.Nausea
5. Peripheral neuropathy
7.Elevated hepatic liver enzyme
9 Hepatic steatosis
18.LeucopeniaContra-indications of DidanosineHypersensitivity to DidanosineSpecial Precautions while taking Didanosine1.Peripheral neuropathy
Pregnancy Related InformationUse with cautionOld Age Related InformationMay be used.Breast Feeding Related InformationUse with cautionChildren Related InformationUse with caution
NEONATES: contraindicatedIndications for DidanosineHIV infectionsInteractions for DidanosineCoadministration of didanosine with drugs that are known to cause pancreatitis may increase the risk of pancreatitis.
Allopurinol: AUC of didanosine increased.
Antacids: Coadministration with antacids containing magnesium or aluminium may potentiate adverse events associated with antacid components.
Ketoconazole/Itraconazole: Should be given at least 2 hours prior to didanosine.
Ganciclovir: May increase steady state AUC of didanosine.
Quinolones: Didanosine should be given 2 hours after or 6 hours before ciprofloxacin.
Typical Dosage for DidanosineAdult: 250 - 400 mg / day
Patient weighing 60 kg or more: 400 mg / day in single or 2 divided dose.
Patient weighing < 60 kg: 250 mg / day in single or 2 divided dose.
Children: 120 mg/sq.metre two times daily
Schedule of DidanosineHStorage Requirements for DidanosineStore it at 15 -25 degree C in a tightly closed container .Protect away from heat and lightEffects of Missed Dosage of DidanosineTake the missed dose as soon as noticed and if it is the time to take the next dose then skip the missed dose and do not double the doseEffects of Overdose of DidanosineGive supportive measures and treatment.
EfavirenzAbout EfavirenzEfavirenz is a non-nucleotide reverse transcriptase inhibitor, Antiretroviral Agent.Mechanism of Action of EfavirenzEfavirenz noncompetitively binds to a site other than catalytic site in the HIV- 1 reverse transcriptase enzyme .This binding will results in a structural change in the enzyme and inhibits its activity i.e. conversion of viral RNA to pro viral DNA and subsequent virus replication
Pharmacokinets of EfavirenzAbsorption: It is absorbed after oral administration. Distribution: It is widely distributed in the body in protein bound form. Metabolism: It is metabolised in the liver to inactive metabolite. Excretion: The drug is primarily excreted through faeces and it is also excreted through urine.Onset of Action for Efavirenz3 - 5 hourDuration of Action for EfavirenzN/AHalf Life of Efavirenz48 hourSide Effects of Efavirenz1.Rash
Contra-indications of EfavirenzHypersensitivity to EfavirenzSpecial Precautions while taking Efavirenz1.Renal impairment
4.Patient with increased cholesterol level and serum transaminases level
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with caution.Breast Feeding Related InformationContraindicated.Children Related InformationUse with caution.
NEONATES: contraindicatedIndications for EfavirenzHIV-1 infectionInteractions for EfavirenzGrapefruit juice may affect plasma efavirenz concentration.
Antibacterials: Increased risk of rash with clarithromycin. Rifampicin reduces plasma concentration of efavirenz.
Antidepressants: Avoid concomitant use of St. John?s Wort (Hypericum perforatum - a long living plant with yellow flowers).
Antihistaminics: Increased risk of ventricular arrhythmias when used with terfenadine.
Other antivirals: Efavirenz reduces plasma concentration of amprenavir, indinavir and lipinavir. Efavirenz reduces plasma concentration of saquinavir.
Anxiolytics: Risk of prolonged sedation with Midazolam.
Oestrogen and Progestogens: Possibly reduced efficacy of oral contraceptives.Typical Dosage for EfavirenzAdults: 600mg once daily along with other antiretroviral agent.
Over 3 years(13-14kg body weight) : 200mg once daily;
15-19kg body weight: 250mg once daily;
20-24kg body weight: 300mg once daily;
25-32.4kg body weight: 350mg once daily;
32.5-39kg body weight: 400mg once daily;
above 40kg body weight:same as adult doseSchedule of EfavirenzHStorage Requirements for EfavirenzStore at 15 - 30 degree C in a tightly closed container. Protect away from heat and light. Keep out of the reach of children.Effects of Missed Dosage of EfavirenzTake the missed dose as soon as noticed and if it is the time to take the next dose then skip the missed doseEffects of Overdose of EfavirenzGive supportive measures and treatment. Activated charcoal can be given to reduce the absorption of the drug
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