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Pharmacology > Block 9 > Flashcards

Block 9 Flashcards

1
Q

Paracetamol
Use
Actions
MOA

A

Use: when NSAIDs cannot be used e.g. peptic ulcer
Action: analgesia + antipyretic
MOA: COX + COX 3 inhibitor (analgesia) hypothalamus -> vasodilation + sweating (antipyretic)

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2
Q

Amoxicillin
Class
Gram +ve/-ve
MOA

A

Beta-lactam antibiotic
Inhibits bacterial cell wall synthesis
Mostly gram +ve some gram -ve

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3
Q

Clauvulanic acid
MOA
Use

A

B-lactamase inhibitor

Combined w/ amoxicillin - overcome antibiotic resistance

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4
Q 
Methicillin
Class
Gram +ve/-ve
MOA
Resistance?
A

Narrow spectrum beta lactam antibiotic
Gram +ve
Transpeptidase inhibitor - Inhibits bacterial cell wall synthesis
MRSA

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5
Q 
Cefuroxime
Class
Gram +ve/-ve
MOA
Considerations
A

Cephalosporin antibiotic
Gram +ve and Gram -ve
Transpeptidase inhibitor - Inhibits bacterial cell wall synthesis
Crosses blood-brain barrier

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6
Q 
Benzylpenicillin
Class
Gram +ve/-ve
MOA
Resistance?
A

Beta lactam antibiotic
Mostly gram +ve some gram -ve
Transpeptidase inhibitor
V. stable against beta lactamases

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7
Q 
Oxytetracycline
Class
Use
Gram +ve/-ve
MOA
A

Broad spectrum antibiotic
Acne
Gram +ve and Gram -ve
30s inhibitor - inhibits translation

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8
Q 
Erthromycin
Class
Use
MOA
Considerations
A

Macrolide antibiotic
Resp inf., syphillis, skin inf., chronic prostatitis,
50s inhibitor - inhibits protein synth
Pregnancy - breast milk + crosses placenta

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9
Q 
Gentamycin
Class
Gram +ve/-ve
Use
MOA
Considerations
A

Broad spectrum aminoglycoside
Mostly gram -ve: pseudomonas, acinetobacter, enterobacter
Some gram +ve
TB
30s/50s inhibitor - inhibits protein synthesis
Ear + Kidney damage

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10
Q 
Rifampacin
Class
Use
Gram +ve/-ve
MOA
A

Broad spectrum antibiotic
TB
Gram +ve and Gram -ve
Inhibits RNA polymerase

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11
Q 
Trimethoprim
Class
Use
Gram +ve/-ve
MOA
A

antibacterial - folate antagonist
UTIs + bronchitis
Gram +ve and Gram -ve
Inhibits dihydrofolate reductase

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12
Q 
Sulfamethoxazole
Class
Use
Gram +ve/-ve
MOA
A

sulfonamide bacteriostatic antibiotic
UTIs, bronchitis, chronic prostatitis, lysteria monocytogenes
Gram +ve and Gram -ve
Dihydrofolate synthesase inhibitor - folate antagonist

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13
Q 
Vancomycin
Class
Use
Gram +ve/-ve
MOA
A

Glycopeptide antibiotic
“Drug of last resort” - Listeria, penicillin res. strep. pn. , strep p. , strep a., actinomyces, lactobacillus sp.,
Gram +ve only
Peptidoglycan inhibitor, also incr. memb. permeability + inhibits RNA synthesis

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14
Q 
Colistin
Class
Use
Gram +ve/-ve
MOA
A

Phospholipid detergent - polymixin antibiotic agent
Multi-drug resistant gram -ve bacteria, v effective against pseudamonas aeruginosa
Incr. bact. memb. permeability + precipitates ribosomes

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15
Q 
Ciprofloxacin
Class
Use
Gram +ve/-ve
MOA
A

Fluoroquinolone antibiotic
Bacterial infections resistant to other antibiotics
Gram +ve and Gram -ve
Topoisomerase II and IV inhibitor - inhibits DNA replication + transcription

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16
Q

Fusidic acid
Class
Gram +ve/-ve
MOA

A 
Bacteriostatic antibiotic
Gram +ve only
Translocation inhibitor (elongation factor g) - therefore inhibiting protein synthesis
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17
Q

Ibuprofen
Class
Action
MOA

A

NSAID
Analgesia
Antipyretic
COX-2 inhibition - reduces prod. of prostaglandins
Antipyretic effects - works on hypothalamus (vasodilation)

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18
Q

Aspirin
Class
Action
MOA

A

NSAID
Analgesia
Antipyretic
Antiplatelet
COX-1 and COX-2 inhibitor (non-selective) - reduces prod of prostaglandins
Platelets - irreversible binding to COX stops prod. of thromboxane A2, effects last 7 to 10 days (lifetime of platelets)

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19
Q 
Acyclovir
Class
Use
Action
MOA
A

Antiviral
Herpes simples
Immunocompromised: varicella zoster and herpes zoster
Inhibits HSV specific DNA polymerases
Nucleoside analogue - converted by viral thymidine kinase

20
Q

Amantadine
Class
Use
MOA

A

Antiviral + Antiparkinsonian
Parkinsons, post-herpetic neuralgia, Infl. A (not reccomended)
Inhibits viral M2 ion channel - required for viral “uncoating”

21
Q 
Amprenavir (pro-drug: fosamprenavir)
Class
Use
MOA
Side effects
A

Antiretroviral
HIV
Protease inhibitor - inhibits HIV-1 protease -> formation of immature virus particles
Hepatic dysfunction

22
Q 
Aspirin
Class
Action
Use
MOA
Side effects
A 
NSAID
Analgesic
Antipyretic
Anti-inflammatory
Antiplatelet
MI, TIA, Stroke, AF, CVD
Irreversibly inhibits COX -> prostaglandins (inc IL-1 mediated realese in hypothalamus)
Antiplatelet - prevents thromboxane A2 synthesis
GI ulcers, haemorrhage, tinnitus
23
Q 
Diamorphine
Class
Use
MOA
Side effects
A

Opioid
Acute/chronic pain
Prodrug -> morphine, binds mu opioid receptors -> analgesia
Cardiorespiratory depression, constipation

24
Q 
Ibuprofen
Class
Use/action
MOA
Side effects
A

NSAID
Analgesic, anti-inflammatory, anti-pyretic
Irreversible COX binding, mainly COX-2 -> decr. prostaglandin prod.
GI ulcer, worsens asthma, cardiovascular events

25
Q 
Naproxen
Class
Use/action
MOA
Side effects
A

NSAID
Analgesic, anti-inflammatory, anti-pyretic
Irreversible COX binding, mainly COX-2 -> decr. prostaglandin prod.
GI ulcer, worsens asthma, cardiovascular events

26
Q 
Phenoxymethylpenicillin (Pen V)
Class
Use
Gram +ve/-ve
MOA
A

Beta-lactam antibiotic
Oral inf., tonsillitis, Otitis media
Mostly gram+ve, narrow spectrum
Pen V = oral form of penicillin, binds PBPs to inhibit cell wall synthesis

27
Q

Zidovudine
Class
Use
MOA

A

Antiretroviral (NRTI)
HIV
Prodrug -> zidovudine triphosphate, a thymidine analogue -> inhibits HIV-1 RT

28
Q

Amphotericin
Class
Use
MOA

A

Antifungal
Systemic fungal inf., Aspergilosis, Leishmaniasis
Binds ergosterol -> formation of pores in cell wall

29
Q 
Artmether
Class
Use
MOA
Side effects
A

Antimalarial
Malaria
Unknown - inhibition of anti-oxidant + metabolic enzymes -> reduced growth of parasite
QT prolongation

30
Q

Clotrimazole
Class
Use
MOA

A

Antifungal
Fungal otitis media + skin inf.
Vaginal + vulvar candidiasis
Inhibits 14-a demthylase which converts lanosterol -> ergosterol, pore formation

31
Q

Fluconazole
Class
Use
MOA

A

Antifungal
Candida balanitis
Vulvovaginal candidiasis
Inhibits 14-a demthylase which converts lanosterol -> ergosterol, pore formation

32
Q

Nystatin
Class
Use
MOA

A

Antifungal
Oral candidiasis
Binds ergosterol, pore formation

33
Q

Pyrimethamine
Class
Use
MOA

A

Antimalarial/folate antagonist
Toxoplasmosis in preg., Malaria
Inhibits dihydrofolate reductase -> reduces tetrahydrofolic acid prod. -> Inhibits DNA and RNA synthesis

34
Q

Quinine
Class
Use
MOA

A

Antimalarial
Choloroquine resistant plasmodium falciparum malaria
Inhibits haem polymerase - parasite can no longer digest haemoglobin -> starves
QT prolongation

35
Q

Clobetasone
Class
Use
MOA

A

Moderate glucocorticoid
Eczema
Anti-inflammatory - prevents expression of cox-1 and cox-2 and prod. of eicosanoids

36
Q

Griseofulvin
Class
Use
MOA

A

Fungal mitosis inhibitor
Dermatophyte infections
Inhibits fungal cell mitosis + nucleic acid synth.
Binds alpha/beta tubulin to inhibit spindle + microtubule function

37
Q

5-fluorouracil
Class
Use
MOA

A

Pyrimidine analogue
GIT + breast tumours (malignant)
Skin lesions (malignant + pre-malignant)

38
Q

Cyclophosphamide
Class
Use
MOA

A 
Alkylating agent
Severe RA
Leukaemias + lymphomas
Active metabolite = aldo phosphamide
Binds to DNA bases causing damage and preventing transcription
39
Q

Dacarbazine
Class
Use
MOA

A

Alkylating agent
Melanoma, Sarcoma, Hodgkin’s disease
Unknown - possibly a purine analogue, possibly binds DNA like normal alkylating agents

40
Q

Doxorubicin
Class
Use
MOA

A

Anticancer - topoisomerase II inhibitor
Leukaemia, Lymphomas, Solid tumours (e.g. breast cancer), Sarcoma, Bladder tumours
Antibiotic w/ antimitotic and cytotoxic properties. Inhibits topoisomerase II -> stops DNA from unwinding

41
Q

Etoposide
Class
Use
MOA

A

Anticancer
Small cell carcinoma, lymphomas, testicular cancer
Topoismerase II inhibitor - cancers depend more heavily on this enzyme, inhibition leads to DNA breakages

42
Q 
Imatinib
Class
Use
MOA
Considerations
A

Tyrosine kinase inhibitor
leukaemias, GI tumours, dermatofibrosarcoma protuberans
In CML, the philadelphia chromosome forms a mutated kinase called Bcr-ABL
Hep B reactivation

43
Q

Paclitaxel
Class
Use
MOA

A 
Anticancer (taxane)
Ovarian + breast cancer
NSCLC
Kaposi's sarcoma
Pancreatic adenocarcinoma
Binds tubulin and induces apoptosis through bcl-2 binding
44
Q 
Rituximab
Class
Use
MOA
Considerations
A 
Anti-CD20 monoclonal antibody
RA patients (where DMARDs = ineffective)
Lymphomas + leukaemias
Binds CD20 receptor on B cells inducing cell lysis
Cardiac events
45
Q 
Tamoxifen
Class
Use
MOA
Considerations
A

SERM
ER positive breast cancer
Gynaecomastia
Anovulatory infertility
Conformational changes to the ER inhibiting oestrogen induced proliferation. Has oestrogenic and anti-oestrogenic effects
Endometrial changes: hyperplasia, polyps, cancer
Thromboembolism risk

46
Q 
Tretinoin
Class
Use
MOA
Considerations
A

Vitamin A analogue
Acute promyelocytic leukaemia
Binds to Retinoic acid receptors (RaRs). RaRa and RaRb linked with acute promyelocytic leukaemia
Retinoic acid syndrome

47
Q 
Vinblastine
Class
Use
MOA
Considerations
A 
Vinca alkaloid
Leukaemias
Lymphomas
Inhibits metaphase -> causes crystallisation of microtubules at mitotic spindle -> cell cycle arrest or apoptosis
Neurotoxicity

Pharmacology (3 decks)

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