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ANTIVIRAL DRUGS Flashcards

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1
Q

REVERSE TRANSCRIPTASE ENZYME IS NEEDED FOR HIV VIRUS TO ___.

A

REPLICATE THE INSIDE OF THE HOST CELLS

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2
Q

2 DRUGS THAT TARGET OR INHIBIT THE REVERSE TRANSCRIPTASE ENZYME ARE:

A
  1. NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR (NRTI)
  2. NON- NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR (NNRTI)
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3
Q

EXAMPLE OF NRTI

A

ZIDOVUDINE
STAVUDINE
ABACAVIR
TENOFOVIR

“STAZ”

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4
Q

EXAMPLES OF NNRTI

A

NEVIRAPINE (“NAVY ERA PIN”)
EFAVIRENZ (“EH FAR GI RUN”)

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5
Q

ZIDOVUDINE IS KNOWN AS

A

AZIDOTHYMIDINE (AZT)

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6
Q

ZIDOVUDINE IS A PRODRUG IN WHICH, WHEN CONVERTED, IT WILL BE

A

TRIPHOSPHATE

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7
Q

THE PK OF ZIDOFUVINE

A

ADMINISTERED ORALLY OR IV
CROSS BBB AND DISTRIBUTED TO CSF
ELIMINATED VIA RENAL
RENAL IMPAIRMENT PATIENTS NEED DOSE THERAPY

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8
Q

MOA OF ZIDOFUDINE

A
  1. NRTI CONVERTED TO ACTIVE TRIPHOSPHATE METABOLITES (NUCLEOTIDES) BY HOST CELL KINASE
  2. NUCLEOTIDES COMPETE WITH ENDOGENOUS NUCLEOSIDE TRIPHOSPHATE TO INCORPORATE INTO VIRAL DNA
  3. ONCE INCORPORATED TO VIRAL DNA, NRTI -> DNA CHAIN TERMINATION
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9
Q

CLINICAL USE OF ZIDOVUDINE

A

1.HIV
2. PREVENT VERTICAL TRANSMISSION OF HIV - FROM MOTHER TO BABY (ADMINISTERED FROM 14TH - 34TH WEEK OF GESTATION)

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10
Q

ADR OF ZIDOFUVINE

A
  1. ACCUMULATE IN DIVIDING CELLS OF THE BODY -> INCREASED TOXICITY OF AZT
    - BONE SUPPRESSION: ANAEMIA, NEUTROPENIA
    - GIT: NAUSEA, ANOREXIA, ABDOMINAL PAIN, HEPATOTOXICITY.
    - CNS: INSOMNIA, ENCEPHALOPATHY, CONVULSION
    - MSK: MYOPATHY
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11
Q

PK OF NEVIRAPINE

A
  • ADMINISTERED ORALLY- GOOD ORAL BIOAVAILABILITY
  • HIGHLY LIPOPHILIC AND WIDELY DISTRIBUTED INCLUDING CSF
  • CYTOCHROME P450 INDUCER -> ACCELERATE CERTAIN DRUG METABOLISM
  • EXTENSIVELY METABOLISED BEFORE BEING EXCRETED IN URINE
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12
Q

MOA OF NEVIRAPINE

A
  1. BIND DIRECTLY TO REVERSE TRANSCRIPTASE AND DISRUPT CATALYTIC SITE
  2. NO PHOSPHORYLATION
  3. NO INCORPORATION INTO VIRAL DNA
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13
Q

CLINICAL USE OF NEVIRAPINE.

A
  1. TREATMENT OF HIV
  2. ACT SYNERGISTICALLY WITH NRTI AND PI
  3. NEVER BEING USED AS SINGLE TX D/T DEV. OF RESISTANCE RAPIDLY.
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14
Q

ADR OF NEVIRAPINE

A
  • RASH
  • NAUSEA
  • HEADACHE
  • STEVEN- JOHNSON SYNDROME
  • HEPATOXICITY
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15
Q

WHAT HAPPEN IF NRTI + NNRTI COMBINED TGT?

A
  • COMBINATION OF THESE DRUG WILL GIVE SYNERGISTIC INHIBITION OF HIV REPLICATION
  • COMBINATION OF NRTI AND NNRTI LEADS TO MORE EFFECTIVE THERAPY.
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16
Q

STATE AN EXAMPLE OF PROTEASE INHIBITOR.

A

RITONAVIR.

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17
Q

STATE THE PK OF RITONAVIR.

A

RITONAVIR IS:
- ADMINISTERED ORALLY
- EXTENSIVELY METABOLISED BY CYP450
- EXCRETED VIA FAECAL

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18
Q

STATE THE MOA OF RITONAVIR.

A

RITONAVIR WILL BIND TO THE ACTIVE SITE OF THE PROTEUS ENZYME -> THEN IT WILL INHIBIT THE PROTEOLYTIC ACTIVITY -> THEREBY IT WILL CAUSE IMMATURE NON INFECTIOUS PARTICLES.

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19
Q

RITONAVIR CAN LEAD TO

A
  1. LIPID ACCUMULATION (LIPODYSTROPHY) AND HYPERLIPIDAEMIA
  2. INSULIN RESISTANCE AND DIABETES
  3. ELEVATED LIVER FX TEST
  4. GIT INTOLERANCE
  5. DDI - CYP3A4 INHIBITOR ( INCREASE DRUG PLASMA CONCENTRATION)
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20
Q

MARAVIROC IS

A

ENTRY INHIBITOR

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21
Q

ENTRY INHIBITOR IS ALSO KNOW AS

A

CCR5 ANTAGONIST

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22
Q

CCR5 ANTAGONIST IS

A

MARAVINOC

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23
Q

MOA OF MARAVINOC

A

MARAVINOC WILL SELECTIVELY AND REVERSIBLY BINDS TO CHEMOKINES CO RECEPTOR (CCR5) WHICH LOCATED ON HUMAN CD4 CELLS -> HENCE IT WILL PREVENT THE INTERACTION WITH THE HIV -1 GLYCOPROTEIN 120

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24
Q

MARAVINOC CAN BE METABOLISED BY

A

CYP3A4

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25
MARAVINOC IS EXCRETED VIA
RENALM
26
MARAVINOC'S HALF LIFE IS
16 HR
27
MARAVINOC CAN BE USE IN
1. ACTIVE AGAINST HIV STRAINS RESISTANT TO REVERSE TRANSCRIPTASE AND PROTEASE INHIBITOR 2. APPROVED FOR HIV INJECTION CAUSED BY DRUG- RESISTANT STAIN 3. ADDITION OF THIS DRUG SHOWED DECREASED VIRAL LOAD, INCREASE CD4 CELLS AND IMPROVE SYMPTOMS
28
MARAVINOC CAN CAUSE
1. HEPATOTOXICITY 2. SKIN REACTION 3. ALLERGIC REACTION
29
FUSION INHIBITOR'S EXAMPLE IS
ENFUVIRTIDE
30
THE MECHANISM OF ACTION OF FUSION'S INHIBITOR IS
FUSION INHIBITORS: ENFUVIRTIDE - BIND TO HIV GLYCOPROTEIN 41 AND PREVENT THE FUSION PROCESS
31
STATE THE PK OF ENFUVIRTIDE
- D/T LARGE STRUCTURE, NOT SUITABLE FOR ORAL ADMINISTRATION - IT IS EFFECTIVE TO BE GIVEN VIA SUBCUTANEOUS INJECTION TWICE DAILY.
32
WHY IS ENFUVIRTIDE IS ADDED TO COMBINATION OF ANTI- HIV DRUG REGIME?
ADDITION OF ENFUVIRTIDE IN REGIMEN SIGNIFICANTLY CAN CAUSE - DECREASE THE VIRAL LOAD - INCREASE THE CD4 COUNT IT PROVIDE ALTERNATIVE TO ANTI- HIV WHEN DRUG RESISTANCE OR INTOLERANCE OCCURS HOWEVER, ENFUVIRTIDE IS NOT THE FIRST LINE TREATMENT.
33
STATE THE ADR OF ENFUVIRTIDE.
SEVERE ALLERGIC REACTION HEAT, SWELLING, REDNESS AND PAIN AT INJECTION SITE
34
RALTEGRAVIR IS AN
INTEGRASE INHIBITOR
35
STATE THE EXAMPLE OF INTEGRASE INHIBITOR
RALTEGRAVIR
36
RALTEGRAVIR PREVENT PROVIRAL DNA STRAND TRANSFER BY BINDING _ IN THE CATALYTIC CORE OF INTEGRASE THAT IS REQUIRED FOR INTERACTION OF ENZYME WITH HOST CELL DNA
RALTEGRAVIR PREVENT PROVIRAL DNA STRAND TRANSFER BY BINDING DIVALENT CATION IN THE CATALYTIC CORE OF INTEGRASE THAT IS REQUIRED FOR INTERACTION OF ENZYME WITH HOST CELL DNA
37
RALTEGRAVIR IS GIVEN
ORALLY TWICE DAILY
38
STATE THE HALF LIFE OF RALTEGRAVIR
9 HRS
39
RALTEGRAVIR IS EXCRETED VIA
URINE IN WHICH 14% IS UNCHANGED
40
STATE THE CLINICAL USE OF RALTEGRAVIR.
RALTEGRAVIR IS - POTENT AGAINST WILD TYPE AND MULTIDRUG- RESISTANT HIV STAIN - USE IN COMBINATION WITH OTHER ANTI-RETROVIRAL DRUGS.
41
STATE THE ADR OF RALTEGRAVIR
NAUSEA AND VOMITING EASY BRUISING INSOMNIA CHANGE OF BODY FAT DISTRIBUTION
42
TRUE/ FALSE: MARAVINOC AND ENFUVIRTIDE ARE EFFECTIVE AGAINST HIV 2.
FALSE MARAVINOC AND ENFUVIRTIDE ARE EFFECTIVE AGAINST HIV 1 ONLY
43
STATE EXAMPLE OF DRUG BASED ON THIS CLASSIFICATION. 1. CCR5 INHIBITOR 2. NNRTI 3. NRTI 4. ENTRY INHIBITOR 5. PROTEASE INHIBITOR 6. INTEGRASE INHIBITOR
1. CCR5 INHIBITOR: MARAVINOC 2. NNRTI: NEVIRAPINE 3. NRTI: STAVODINE 4. ENTRY INHIBITOR: MARAVINOC 5. PROTEASE INHIBITOR: RITONAVIR 6. INTEGRASE INHIBITOR: RALTEGRAVIR
44
STATE THE BENEFITS OF COMBINED ARTS
- INCREASE EFFICIENCY - PROLONG PT SURVIVAL - PREVENT HIV RESISTANCE
45
HOW TO MONITOR THERAPY RESPONSE?
1. MEASURE VIRAL LOADS 2-8 WEEKS AFTER START 2. EVALUATE CD4 CELL COUNTS
46
WHAT ARE THE CHALLENGES IN TREATING HIV PT WITH ARTs?
- HIGH RISK OF DDI - HIV CANNOT BE ERADICATED COMPLETELY, THEREFORE, IT NEED LIFE LONG TX - TX FAILURE: PT NEED AT LEAST NEW DRUG REGIMEN WHICH INCLUDE 2 NEW DRUGS. - TOXICITY
47
WHAT ARE THE EXAMPLE OF THE HERPES VIRUS?
1. HERPES SIMPLEX VIRUS 2. VARICELLA ZOSSTER VIRUS 3. CYTOMEGALOVIRUS
48
MOST OF THE TX FOR HERPES VIRUS ARE
NUCLEOSIDE ANALOGUE
49
NUCLEOSIDE ANALOGUE USED FOR HERPES INFX HAVE
NATURAL PURINE OR PYRIMIDINE BASE COMBINED WITH SYNTHETIC CARBOHYDRATE MOIETY
50
NUCLEOSIDE ANALOGUE ARE PRODUG/ ACTIVE DRUG
PRODRUG
51
STATE AN EXAMPLE OF DRUG THAT HAS NUCLEOSIDE ANALOGUE
ACYCLOVIR
52
TRUE/FALSE: REGARDING ACYCLOVIR: A. AN ALKALYTIC B. MOSTLY TAKEN UP BY INFECTED CELLS. C. CAN BE GIVEN VIA ORAL ROUTE ONLY D. CAN BE DISTRIBUTED INTO THE CSF E. EXCRETED VIA RENAL SECRETION
A. AN ALKALYTIC FALSE- ACYCLOVIR IS A NUCLEOSIDE ANALOGUE THAT IS USED TO TREAT HERPES INFX B. MOSTLY TAKEN UP BY INFECTED CELLS. TRUE - HENCE THE LOW TOXICITY FOR NORMAL HOST CELLS C. CAN BE GIVEN VIA ORAL ROUTE ONLY FALSE- IT CAN BE GIVEN VIA: ORAL, IV, TOPICAL D. CAN BE DISTRIBUTED INTO THE CSF TRUE- IT CAN BE DISTRIBUTED WIDELY E. EXCRETED VIA RENAL SECRETION TRUE
53
DESC THE MOA OF ACYCLOVIR.
ACYCLOVIR IS A PRODRUG THEREBY IT WILL BE CONVERTED TO ACYCLOVIR MONOPHOSPHATE VIA VIRUS ENCODED THYMIDINE PHOSPHATE. THEN THE ACYCLOVIR MONOPHOSPHATE WILL BE CONVERTED INTO ACYCLOVIR TRIPHOSPHATE WTH THE HELP FROM THE HOST KINASE. ACYCLOVIR TRIPHOSPHATE WILL PRODUCE ACTIVE METABOLITE -> COMPETE WITH THE ENDOGENOUS NUCLEOSIDE. THEREBY IT WILL COMPETITIVELY INHIBIT THE DNA POLYMERASE -> DNA CHAIN TERMINATION
54
STATE THE USE OF ACYCLOVIR.
- TX FOR HSV AND VZV SUCH AS CHICKEN POX, SHINGLES, HERPES GENITALIS, HERPETIC ENCEPHALITIS AND MUCOCUTANEOUS INFX - SUITABLE FOR PROPHYLAXIS OF CMV BUT INEFFECTIVE AS TX OF CMV AND BM/ ORGAN TRANSPLANT REJECTION - HIV INFX PT INFECTED WITH HSV
55
STATE THE ADR OF ACYCLOVIR.
- GI DISTURBANCE - RASH - RENAL TOXICITY - HEADACHE
56
BENEFITS OF ACYCLOVIR.
- PREVENT REPLICATION - REDUCE PAIN - SHORTEN DURATION OF ILLNESS - REDUCE AMOUNT OF VIRAL SHEDDING
57
ACYCLOVIR DOES NOT ELIMINATE THE VIRUS FOR HERPES GENITALIS BUT WHY DO WE STILL TREAT WITH ACYCLOVIR?
- IT IS STILL ADMINISTERED BECAUSE IT CAN: 1. REDUCE PAIN 2. SHORTEN DURATION OF ILLNESS 3. REDUCE THE AMOUNT OF VIRAL SHEDDING
58
STATE ONE EXAMPLE OF ANTI- INFLUENZA DRUG THAT IS NEURAMINIDASE INHIBITOR.
OSELTAMIVIR
59
MOA OF OSELTAMIVIR
BINDS TO ACTIVE SITE -> INHIBIT THE ENZYME NEURAMINIDASE IN INFLUENZA A AND B -> 1. PREVENT VIRION RELEASE FROM SURFACE OF INFECTED CELLS 2. PREVENT VIRION SPREAD BY INACTIVATING MUCUS
60
TRUE/ FALSE: REGARDING OSELTAMIVIR: A. IT IS ADMINISTERED THROUGH IV ROUTE B. IT CAN TREAT ONLY INFLUENZA A C. IT HAS MINOR RESPIRATORY SYMPTOMS AND GIT SYMPTOMS D. IT IS TOLERATED BETTER THAN AMANTADINE E. IT IS USED AS PROPHYLAXIS IN CHD.
A. IT IS ADMINISTERED THROUGH IV ROUTE FALSE - OSELTAMIVIR IS ADMINISTERED VIA ORAL ROUTE ONLY. B. IT CAN TREAT ONLY INFLUENZA A FALSE- IT CAN TREAT BOTH INFLUENZA A AND B. C. IT HAS MINOR RESPIRATORY SYMPTOMS AND GIT SYMPTOMS TRUE D. IT IS TOLERATED BETTER THAN AMANTADINE TRUE E. IT IS USED AS PROPHYLAXIS IN CHD. TRUE- IT ALSO BEING USED AS PROPHYLAXIS IN CHRONIC LIVER, RENAL, NEUROLOGICAL DISEASE AS WELL AS DM.
61
STATE THE CLINICAL USE OF OSELTAMIVIR.
1. TREATMENT FOR BOTH INFLUENZA A AND B IN WHICH IT IS ADMINISTERED WITHIN 48 HRS OF SYMPTOMS TO REDUCE THE SEVERITY AND DURATION OF ILLNESS 2. AS A PROPHYLAXIS IN - CHD - CHRONIC LIVER DISEASE - CKD - CHRONIC NEUROLOGICAL DISEASE - DM
62
OTHER THAN OSELTAMIVIR, STATE ONE EXAMPLE OF NEURAMINIDASE INHIBITOR DRUG.
ZANAMIVIR
63
STATE THE MOA AND PK OF ZANAMIVIR
MOA: ZANAMIVIR WILL INHIBIT THE NEURAMINIDASE PROTEIN -> ALTER VIRUS PARTICLE AGGREGATION AND VIRUS RELEASE PK: - POOR ORAL BIOAVAILABILITY - IN POWDER FORM (INHALE) - EXCRETED URINE (UNCHANGED) - T1/2 - 2-5 HRS
64
ZANAMIVIR CAN TREAT ___
BOTH INFLUENZA A AND B
65
AMANTADINE IS USED TO TREAT ___.
INFLUENZA A PARKINSON POSTHERPETIC NEURALGIA
66
HOW AMANTADINE TREAT PARKINSON PT?
- AMANTADINE IS ANTI-PARKINSON AGENT IN WHICH IT IS USED TO TREAT THE EXTRAPYRAMIDAL REACTION. - IT WILL INCREASE THE DOPAMINE RELEASE IN THE BRAIN BUT DOES NOT POSSESS ANTICHOLINERGIC ACTIVITY.
67
MOA OF AMANTADINE
AMANTADINE WILL PREVENT THE VIRAL UNCOATING BY BLOCKING M2 PROTON SELECTIVE ION CHANNEL -> PREVENT TRANSFER OF VIRAL NUCLEIC ACID INTO THE HOST CELL CYTOPLASM.
68
TRUE/FALSE: AMANTADINE IS ADMINISTERED VIA ORALLY.
TRUE
69
STATE THE ADR AND CLINICAL USE OF AMANTADINE.
ADR: 1. CNS- CONFUSION 2. INSOMNIA 3. DIZZINESS CLINCAL USE: PROPHYLAXIS AND TX OF INFLUENZA A ONLY

PHARMACOLOGY (9 decks)

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