Drug Interaction:
Interacting drugs- summary
+ Saquinavir-
Ketoconazole
concomittant admin resulted in steady-state saquinavir AUC and
Cmax values . No dosage adjustment is required
Rifampin
coadmin of rifampin decreased the steady-state AUC and Cmax of
saquinavir by 80%, Steady-state AUC of siquinavir was deceased
by 40% when saquinavir was coadministered with rifabutin
Indication:
Approved by the FDA on December 1995
LIST OF DRUGS DURING 2006
Sr.No- 27
Name of the Drug- Saquinavir (500mg) tablet (addl.Stgth) Pharmacological Classification- Anti-AIDS
Date of Approval- 20-03-2006
Approved by U.S.FDA on 30-12-2006 (Ref- FDA approved List- 2006)
New Drugs Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
1.Saquinavir HIV/AIDS August 1997
2.Squinavir 500mg tablet ANTI-AIDS 20-03-2006
Addl.Stgth
Patent Expiry Date of drugs (Ref - IDMA Publication)
Chemical Category Manufacturer/ US Patent
Ingredient- Marketer Expiration Date
Saquinavir HIV/AIDS Roche 19-11-2010
Pharmacological Classification- Anti-AIDS
Date of Approval- 20-03-2006
Approved by U.S.FDA on 30-12-2006 (Ref- FDA approved List- 2006)
New Drugs Approved by (DCI) Drug Controller GENERAL - India For Marketing
(Ref- IDMA Publication)
Name of Drug Indication Date of Approval
1.Saquinavir HIV/AIDS August 1997
2.Squinavir 500mg tablet ANTI-AIDS 20-03-2006
Addl.Stgth
Patent Expiry Date of drugs (Ref - IDMA Publication)
Chemical Category Manufacturer/ US Patent
Ingredient- Marketer Expiration Date
Saquinavir HIV/AIDS Roche 19-11-2010
Adverse Reaction:
Majority of adverse reactions were of mild intensity
Most frequently reported adverse events among patients reported were-
Diarrhea, abdominal discomfort, and nausea.
Rare occurences of the following serious adverse reactions-
Confusion, ataxia, and weakness, acute myeloblastic leukemia, hemolytic anemia,
attempted suicide Stevens Johnson syndrome, seizures, severe cutaneous reactions, associated with increased liver function tests, isolated elevation of transaminase,
thrombophebitis, headache, and thrombocytopenia
Contra-Indications:
Hypersens to the drug
Special precautions:
Hepatic function impairment, pregnancy, lactation, children
Toxicity- if a serious or severe toxicity occurs during treatment with squinavir,interupt therapy until the etiology of the event is identified or the toxicity resolves
Monitoring- Perform clinical chemistry tests prior to initiating saquinavir therapy and at appropiate intervals thereafter.
Warnings-
Hepatic function impairment- excercise caution when administering saquinavir to patients with hepatic insufficiency because patients liver function tests > 5 times the normal upper limit were not included in clinical studies.
Pregnancy- use during pregancy after taking account the importance of the drug to the mother.
Lactation- Decide whether to discontinue nursing or discontinue the drug taking into account the importance of the drug to the mother.
Children- safety and efficacy in HIV treated children or adolescents < 16 years of age have not been established.
Dosages/ Overdosage Etc:
Approved by the FDA on December 1995
Indications:
HIV infections
Dosage:
Recommende dosage in combination with a ne\ucleoside analog is three 200mg capsules 3 times daily within 2 hours after a full meal.
Overdosage- Symptoms No acute toxicities were noted in one patient who ingested 8g saquinavir as a single dose.
Treatment
1. Patient was treated with induction of emesis within 2 to 4 hours after ingestion
Missed dose-
1. If you miss a dose of this medicine, take it as soon as possible.
2. However, if it is almost time for next dose, skip the missed dose and go back to your regular dosing schedule.
3. Do not double doses.
Other Information:
EVIDENCE BASED MEDICINE (MIMS April 2003)
Post-herpetic Neuralgia
Comparitive effectiveness of various interventions
Prevention of post-herpetic neuralgia
Beneficial
1. Oral antiviral agents such as acyclovir, famciclovir, valaciclovir, netivudine
2. Tricyclic antidepressants (amitriptyline)
Unknown effectiveness
1. Levodopa 2. Amantadine 3. Isoprinosine 4. Adenosine monophosphate
Unlikely to be beneficial
1. Topical antiviral agents (idoxurine) for relief of acute oain only
2. Cimetidine Ineffective or harmful 1. Corticosteroids Relieving established post-herpetic neuralgia
Beneficial
1. Tricyclic antidepressants (amitriptyline)
2. Oxycodone (opiod)
3. Gabapentin (anticonvulasant)
Unknown effectiveness
1. Capsaicin (topical counterirritant)
2. Topical lignocaine
Ineffective or harmful
1. Epidural morphine
2. Dextromethorphan
KEY POINTS
1. Daily acyclovir reduced the relative risk of of post-herpetic pain at six months by about 50 % compared with placebo
2. Famciclovir significantly reduced pain duration after acute herpes zoster.
3. Idoxuridine was associated with short term pain relief in acute herpes zoster but did not prevent post-herpetic neuralgia
4. Conflicting evidence on whether corticosteroids alone prevent post-herpetic neuralgia. Limited evidence that high dose steroids and antiviral agents combined may speed healing of acute zoster. No evidence that it reduces post-herpetic neuralgia
5. Amitriptyline started during the acute episode reduced prevalence of post-herpetic neuralgia at six months.
6. Insufficient evidence on the effect of other drug tretment.
Patient Information:
1. Inform patients that Saquinavir is not a cure for HIV infection and that they may acquire illness associated with advanced HIV infection
2. Tell patients that long term patients of saquinavir are not known
3.Advise patients that saquinavir should be taken within 2 hours after a full meal.
Pharmacology/ Pharmacokinetics:
Pharmacology:
Saquinavir is an inhibitor of the human immunodefiency virus(HIV) protease. HIV prorease cleaves viral polyprotein precursors to generate functional proteins in HIV infected cells.
Pharmacokinetics:
Following multiple dosing (600mg 3 times daily) in HIV infevted patients, the staedy-state area under the plasma conc curve (AUC) was 2.5 times higher than observed after a single dose.
Interaction with Food:
To be taken within 2 hours after a meal.
Pregnancy and lactation:
Pregnancy:
Use during pregnancy, taking into account the importance of the drug to the mother
Lactation:
Use with caution and decide whether to discontinue the drug or the discontinue nursing taking into account the importance of the drug to the mother.
Children-
Safety and efficacy in HIV treated children or adolescents < 16 years of age have not been established.
