Pharmacology Flashcards

1
Q

Atazanavir

A

CYP34A Strong inhibitor HIV Protease inhibitor used for PEP

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2
Q

Boceprevir

A

CYP34A Strong inhibitor HCV genotype 1 protease inhibitor

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3
Q

Clarithromycin

A

CYP34A Strong inhibitor

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4
Q

Cobicistat

A

CYP34A Strong inhibitor In combination with other HIV drugs to increase the levels

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5
Q

Darunavir

A

CYP34A Strong inhibitor HIV protease inhibitor

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6
Q

Idelalisib

A

CYP34A Strong inhibitor phosphoinositide 3-kinase inhibitor Treats relapsed CLL in combo with Ritux

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7
Q

Indinavir

A

CYP34A Strong inhibitor HIV protease inhibitor

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8
Q

Itraconazole

A

CYP34A Strong inhibitor

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9
Q

Ketoconazole

A

CYP34A Strong inhibitor

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10
Q

Lopinavir

A

CYP34A Strong inhibitor HIV protease inhibitor

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11
Q

Mifepristone

A

CYP34A Strong inhibitor antiprogestogen - competitive

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12
Q

Nefazodone

A

CYP34A Strong inhibitor atypical antidepressant (not used much)

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13
Q

Nelfinavir

A

CYP34A Strong inhibitor HIV protease inhibitor

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14
Q

Ombitasvir-paritaprevir-ritonavir

A

CYP34A Strong inhibitor HCV

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15
Q

Posaconazole

A

CYP34A Strong inhibitor

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16
Q

Saquinavir

A

CYP34A Strong inhibitor HIV protease inhibitor

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17
Q

Telaprevir

A

CYP34A Strong inhibitor HCV protease inhibitor

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18
Q

Telithromycin

A

CYP34A Strong inhibitor Ketolide / macrolide antibiotic

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19
Q

Voriconazole

A

CYP34A Strong inhibitor

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20
Q

Amiodarone

A

CYP34A inhibitor

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21
Q

Aprepitant

A

CYP34A inhibitor

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22
Q

Cimetidine

A

CYP34A inhibitor histamine H₂ receptor antagonist

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23
Q

Conivaptan

A

CYP34A inhibitor non-peptide inhibitor of antidiuretic hormone (vasopressin). It was approved in 2004 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH)

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24
Q

Crizotinib

A

CYP34A inhibitor ALK TKI (ALK + NSCLC) Criz.. Crazy rich asians get ALK (Asian Lung Kancer)

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25
Q

Cyclosporine

A

CYP34A inhibitor

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26
Q

Diltiazem

A

CYP34A inhibitor

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27
Q

Duvelisib

A

CYP34A inhibitor Dual inhibitor of PI3Kδ and PI3Kγ Haem malignancies Du.. dual inhibitor vel..phosphokinase

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28
Q

Dronedarone

A

CYP34A inhibitor like amiodarone

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29
Q

Erythromycin

A

CYP34A inhibitor

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30
Q

Fluconazole

A

CYP34A inhibitor

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31
Q

Fosamprenavir

A

CYP34A inhibitor

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32
Q

Grapefruit juice

A

CYP34A inhibitor

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33
Q

Imatinib

A

CYP34A inhibitor

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34
Q

Isavuconazole

A

CYP34A inhibitor

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35
Q

Letermovir

A

CYP34A inhibitor

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36
Q

Netupitant

A

CYP34A inhibitor

37
Q

Nilotinib

A

CYP34A inhibitor

38
Q

Ribociclib

A

CYP34A inhibitor Cyclin-dependent kinase inhibitor that is used in combination with aromatase inhibitors for breast cancer

39
Q

Schisandra / magnolia berry

A

CYP34A inhibitor

40
Q

Verapamil

A

CYP34A inhibitor

41
Q

Apalutamide

A

CYP34A inducer Antiandrogen Like enza-LUTAMIDE

42
Q

Carbamazepine

A

CYP34A inducer

43
Q

Enzalutamide

A

CYP34A inducer

44
Q

Fosphenytoin

A

CYP34A inducer

45
Q

Lumacaftor

A

CYP34A inducer INDUCES CFTR proteins to treat CF LumaCaFToR

46
Q

Mitotane

A

CYP34A inducer steroidogenesis inhibitor and cytostatic antineoplastic medication which is used in the treatment of adrenocortical carcinoma and Cushing’s syndrome

47
Q

Phenobarbital

A

CYP34A inducer

48
Q

Phenytoin

A

CYP34A inducer

49
Q

Primidone

A

CYP34A inducer anticonvulsant of the barbiturate class

50
Q

Rifampin

A

CYP34A inducer

51
Q

Bexarotene

A

CYP34A inducer It is a third-generation retinoid to treat cutaneous T cell lymphoma bexaROTENE betacaroene

52
Q

Bosentan

A

CYP34A inducer Dual endothelin receptor antagonist

53
Q

Dabrafenib

A

CYP34A inducer B-RAF inhibitor

54
Q

Dexamethasone

A

CYP34A inducer

55
Q

Efavirenz

A

CYP34A inducer non-nucleoside reverse transcriptase inhibitors (NNRTIs)

56
Q

Eslicarbazepine

A

CYP34A inducer

57
Q

Etravirine

A

CYP34A inducer non-nucleoside reverse transcriptase inhibitors (NNRTIs)

58
Q

Modafinil

A

CYP34A inducer

59
Q

St. John’s wort

A

CYP34A inducer

60
Q

Drugs that follow zero order kinetics

A

Zero WHATS Warfarin Heparin Alcohol Theophyline Salicylates

61
Q

CYP3A4 main inhibitors

A

GRACE

Grapefruit
Ritonavir (Protease inhibitors)
Azole antifungals
Calcium channel blockers (verapamil/diltiazam)
Erythromycin/clarithromycin (macrolides)

62
Q

CYP3A4 main inducers

A

CRP - DDB SN

Carbamazepine Rifampicin Phenytoin

Dexamethasone, Dabrafinib (other TKIs are inhibitors), Bosentan

St John’s Wart, NNRTIs

63
Q

P-glycoprotein substrates

A

CA DAMP

Calcineurin inhibitor
Amlodipine

Digoxin
Anti-neoplastics: docetaxal, etoposide, vincristine Macrolides
Protease inhibitors

64
Q

CYP3A4 substrates

A

WC - PCOS & macrolides

Warfarin & DOACS
Carbemazeopine

Protease inhibitors
Calcium channel inhibitors
Opiates & benzos
Statins
Macrolides

65
Q

P-glycoprotein inhibitors

A

MVP

Macrolides
Verapamil
Protease inhibitors

66
Q

P-glycoprotein inducers

A

St John’s Wart
Rifampicin

67
Q

CYP2D6 substrates

A

Got C Phaff

Gefitinib
Olanzapine
Tamoxifen
Codeine
Propranolol
Haloperidol
Amitriptyline
Flecanide
Fluoxetine

68
Q

CYP2D6 inhibitors

A

ABCDM

Amiodarone
Abiraterone
Cobicistat
Duloxetine/fluoxetine
Mirabigron

69
Q

Which antiepileptic causes visual field changes?

A

Vigabatrin Wt gain, visual field changes, drowsiness and neuropsychiatric symptoms

70
Q

Which AED causes the most SJS?

A

Lamotragine Carbamazepine - HLAB*1502

71
Q

Which AEDs are inducers of CYP3A4? ie decreases effect of OCP and cyclosporin

A

Carbamazepine Phenytoin Phenobarbital Na Valproate is safe w OCP (it is a CYP2C9 inhibitor)

72
Q

COMPT inhibitors?

A

Entacapone Tolcapone Prolong dopamine activity by inhibit breakdown of levadopa Therefore extending the dose / stabilising plasma concentration useful for treating pts with motor fluctuations SEs: dopaminermgic + diarrhoea, orange urine

73
Q

Highest risk factor for stroke?

A

Age risk doubles each successive decade after 55

74
Q

Highest modifiable risk factor for stroke?

A

HTN Rx 33-44% risk reduction

75
Q

Charcot Mary Tooth

A

Hereditary sensory motor neuropathy Distal weakness > sensory - Peripheral neuropathy (glove and stocking) Pes cavus foot deformity HSMN 1 - hypertrophic myelin, onion bulbs (slow NCV) with secondary axonal degeneration HSMN2 - neuronal type degeneration (normal NCV)

76
Q

Carbamazepine

A

NA Channel

CYP3A4 substrate and inducer

Indicated for partial seizures

Can worsen myoclonus or absebce seizures

Concentration dependent SEs Diplopia, dizziness, drowsiness, nausea

Idiosyncratic: Rash, SJS

Hyponatraemia

77
Q

Leviteracetam

A

Inhibits presynaptic calcium channels, neuromodulating transmitter release

<10% porotein bound

Renally excreted

Minmal interactions

SEs: sedations, psychosis

78
Q

Phenytoin

A

Sodium channel

non-linear kinetics

90% bprotein bound, displaced in states of hypoalbuminaemia

Met CYP2C9 exc bile and urine

Interactions:
Inhibitors: fluoxetine, fluconazole, isonizid, tamoxifen, amiodarone

Inducers: Rifampicin, chronic EtOH

79
Q

SIde effects of phenytoin

A

Concentration dependent:

ataxia, nystagmus, headache, incoordination, sedation

Idiosyncratic:

Blood dyscrasias, rash, immunological

Chronic:

Cerebellar syndrome, skin thickening, hirsuitism, acne, done disease, folate deficiency

80
Q

Sodium valproate

A

PIP3 reduction, sodium channel, increases GABA

90% protein bound

Met: liver CYP 2C9

inducers: clobazam, stiripentol

Inhibitors: rifampicin, cisplatin, MTX, carbopenums, topiramate

81
Q

Side effects of sodium valproate

A

Concentration dependent:

GI, sedation, thrombocytopenia, tremor, avoid in mitochondrialopathies

Idiosyncratic:

acute hepatic failure, pancreatitis, alopecia

Chronic: tremor, ataxia, weight gain, PCOS

82
Q

Key CYP3A4 substrates:

A

Carbamazipine

Macrolides

Benzodiazepines

Protease inhibitors

Calcium channel blockers

Warfarin

83
Q

CYP2C19 key substrates

A

PPPDW - *Important for 19year olds not to get pregnant

Progesterone
Phenytoin
PPIs
Diazepam
Warfarin

84
Q

CYP2C19 key inhibitors

A

If the 19 year old gets pregnant she’ll need..

SSRIs
PPIs

85
Q

CYP2C19 inducers

A

*Not rifampicin

Carbamazepine

86
Q

CYP2C9 key substrates

A

NAWPS

NSAIDs
ARBs
Warfarin
Phenytoin
Sodium Valproate

87
Q

CYP2C9 key inhibitors

A

FAT

Fluconazole

Amiodarone

Topiramate

CYP2C9 - NAWPS FAT RClobezam

88
Q

CYP2C9 key inducers

A

Rifampicin
Clobezam

CYP2C9 - NAWPS FAT RClobezam