Emerging “CCR5 ANTAGONISTS” Promising HIV Therapeutic Strategy

Presented By; Mahesh Shahi
3rd semester
Bachelor in Pharmaceutical
sciences,CCT
Emerging
“CCR5 ANTAGONISTS”
Promising HIV Therapeutic Strategy
t
Saturday, December 17,Saturday, December 17, 2016

Saturday, May 07, 2016
Pharmaceutical seminar~ 2nd
Contents
1. Quick review about HIV/AIDS
2. Treatment
3. Introduction
4. Chemistry
5. Mechanism of action of Maraviroc
6. Pharmacokinetics
7. Indications
8. Contraindications
9. Side effects
10. Drug Interactions
11. Doses
12. Precautions
13. Dosage forms
14. Storage
15. Conclusion
1
2

Saturday, December 17, 2016
Quick Review of the HIV/AIDs
2
INTRODUCTION HISTORY
TRANMISSION SYMPTOMS
TREATMENT
3

Saturday, December 17, 2016 3
4
Contd…

TREAMENT
5
CCR5 ANTAGONISTS
CONCEPTDISCOVERY

INTRODUCTION
6

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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7
INDICATION
8

8
Life cycle of HIV virus inside Host

MECHANISM OF ACTION
Saturday, December 17,
2016
9

PHARMACOKINECTICS
Bioavailability
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
11

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.

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 day
13

SIDE EFFECTS
1. Less Common
Difficulty having a bowel movement (stool)
Difficulty with moving
Increased or decreased appetite
2. More Common
Stomach discomfort or upset
Loss of interest or pleasure
Unusual tiredness
3. Rare
Convulsion
Vomiting of blood
Loss of voice
Difficulty with breathing
14

CONTRAINDICATION
15

DRUG INTERACTION
 Clarithromycin
Increase Plasma Concentration
 Ketoconazole
Increase Plasma Concentration
 Carbamazepine
Decrease Plasma Concentration
16

PRECAUTIONS
 Kidney problems
 Liver problems
 Alcohol
 Low Blood Pressure
 Hypersentivity
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DOSAGE FORMS
 Tab. : 150,300 & 600 mg
18

STORAGE
 Tab.
 Room temp. – below 15 - 30 c
 Protect from Sunlight and Moisture
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CONCLUSION
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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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Emerging “CCR5 ANTAGONISTS” Promising HIV Therapeutic Strategy

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