Post on 07-Jan-2017
Presented By; Mahesh Shahi
3rd semesterBachelor in
Pharmaceutical sciences,CCT
Emerging “CCR5 ANTAGONISTS”
Promising HIV Therapeutic Strategy
t
Tuesday, May 2, 2023Tuesday, May 2, 2023
Saturday, May 07, 2016 Pharmaceutical seminar~ 2nd
Contents1. Quick review about HIV/AIDS2. Treatment3. Introduction 4. Chemistry5. Mechanism of action of Maraviroc6. Pharmacokinetics7. Indications8. Contraindications9. Side effects10. Drug Interactions11. Doses12. Precautions13. Dosage forms14. Storage15. Conclusion
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Quick Review of the HIV/AIDs
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INTRODUCTION HISTORY
TRANMISSION SYMPTOMS
TREATMENT3
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CCR5 ANTAGONISTS
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APLAVIROC
VICRIVIROC
MARAVIR
OC
Contd…
DRUGS
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TREAMENT
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CCR5 ANTAGONISTS
CONCEPT
DISCOVE
RY
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INTRODUCTION
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As CCR5 ANTAGONISTFDA approved – Auguest 6, 2007
Combination with HAART
Labeled – only in CCR5 Tropic
Selzentry - USACelsentric – Europe, Sep. 2007
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CHEMISTRY Formula = C29H41F2N5O
Molecular mass = 513.666 g/mol
IUPAC name = 4,4-difluoro-N-{(1S)-3-[3-(3-isopropyl- 5-methyl-
4H-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]oct-8-yl]-1-
phenylpropyl}cyclohexanecarboxamide
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INDICATION
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Blocking the HIV virus from entering
Lowers the HIV complications
Decrease the risk of spreading
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Life cycle of HIV virus inside Host
MECHANISM OF ACTION
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PHARMACOKINECTICSBioavailability First-pass metabolism systemic availability 23% Protein binding ~ 76%Metabolism Hepatic Biological Life 0.5 to 4 hours Excretion Rectal/Renal Half-Life Elimination 14 – 18 hours
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DOSE CATEGORY AGE GROUP DOSE
Younger below 18 year
Not Available
Adult Above 18 year
Available
Geriatric Above 65 year Not Available
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Note: Use: In combination with other antiretroviral agents, for patients infected with only CCR5-tropic HIV-1.Pharmaceutical seminar~ 2nd
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DOSE IN DETAIL With Potent CYP450 3A Inhibitors(e.g Nefazodone,
Clarithromycin)
150 mg orally twice a day With Other Concomitant Medications (e.g Nevirapine,
Raltegravir, all NRTIs etc
300 mg orally twice a day With potent CYP450 3A Inducers (e.g Carbamazepine,
Phenobarbital)
600 mg orally twice a day13
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SIDE EFFECTS1. Less CommonDifficulty having a bowel movement (stool) Difficulty with moving Increased or decreased appetite2. More CommonStomach discomfort or upset Loss of interest or pleasure Unusual tiredness
3. RareConvulsionVomiting of blood
Loss of voice Difficulty with breathing
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CONTRAINDICATION
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Hepatic impairment
Renal impairment
Cardiovascular disease
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DRUG INTERACTION Clarithromycin
Increase Plasma Concentration
Ketoconazole
Increase Plasma Concentration
Carbamazepine
Decrease Plasma Concentration
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PRECAUTIONS Kidney problems
Liver problems
Alcohol
Low Blood Pressure
Hypersentivity
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DOSAGE FORMS Tab. : 150,300 & 600 mg
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STORAGE Tab.
Room temp. – below 15 - 30 c Protect from Sunlight and Moisture
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CONCLUSIONPrevention is better
than cure !!! –no way…
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REFERENCES Tripathi KD (2008) Essential Medical Pharmacology (6th Ed.), Jaypee Brothers
Publishers Private Limited, New Delhi, India, pp (770-776).
Katzung BG (2007) Basic and Clinical Pharmcology (10th Ed.), McGraw-Hill Medical,
New York, USA, pp (798-811).
URL 1: https://en.wikipedia.org/wiki/Maraviroc (Assessed on: April 28, 2016).
URL 2: http://www.drugs.com/mtm/maraviroc.html (Assessed on: May 4, 2016).
URL 3: http://www.medscape.com/hiv (Assessed on: May 4, 2016).
URL 4 : https://retrovirology.biomedcentral.com/articles/10.1186/1742-4690-10-43
(Assessed on: May 8, 2016).
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Presented by;MAHESH SHAHI 22
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