Emerging “CCR5 ANTAGONISTS” Promising HIV Therapeutic Strategy

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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Tuesday, May 2, 2023

Quick Review of the HIV/AIDs

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INTRODUCTION HISTORY

TRANMISSION SYMPTOMS

TREATMENT3

Pharmaceutical seminar~ 2nd


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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

7Pharmaceutical seminar~ 2nd

Tuesday, May 2, 2023 Pharmaceutical seminar~ 2nd

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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



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



2223


Emerging “CCR5 ANTAGONISTS” Promising HIV Therapeutic Strategy

Health & Medicine