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B4W2 > PHARMACOLOGY > Flashcards

PHARMACOLOGY Flashcards

1
Q

what drug class is azathioprine?

A

an antagonist of purine metabolism/ an immunosuppressant

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2
Q

what does azathioprine do?

A

it acts to inhibit purine synthesis which inhibits DNA and RNA synthesis which leads to an inhibition in cell proliferation. This leads to a decrease in production in white blood cells leading to immunosuppression.

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3
Q

what is immunosuppression?

A

prevention or weakening the body’s ability to produce an immune response

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4
Q

what is azathioprine’s mechanism of action?

A

incorporation of thiopurine analogues into DNA structures which causes chain termination and cytotoxicity.

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5
Q

what are some indications of azathioprine?

A

autoimmune conditions, arthritis, Crohn’s disease, transplant rejection, high TMPT activity, myasthenia gravis

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6
Q

what is TMPT? what does it do?

A

thiopurine S-methyltransferase.

it breaks down thiopurine drugs which suppress the immune system.

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7
Q

what are the side effects of azathioprine?

A

bone marrow depression, increased risk of infection, leucopenia, pancreatitis and thrombocytopenia.

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8
Q

what should azathioprine not be given in conjunction with?

A

purine analogues (antimetabolites that mimic the structure of metabolic purines)

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9
Q

what must be monitored with long term treatment with azathioprine?

A

blood tests and monitoring for signs of myelosuppression

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10
Q

what drug class is cyclosporin?

A

an immunosuppressive agent/ a cyclophilin binder

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11
Q

what is the mechanism of cyclosporin?

A

it binds to cyclophilin which causes inhibition of calcineurin which is responsible for activating the transcription of IL-2. this causes the reversible inhibition of immunocompetent lymphocytes in the G0 or G1 phase of the cell cycle. T lymphocytes are preferentially inhibited.

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12
Q

what are the indications of cyclosporin?

A

organ and bone marrow transplantation

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13
Q

what are the common side effects of cyclosporin?

A

eye inflammation, appetite decreased, diarrhoea, fatigue, fever, flushing, GI discomfort, trembling, vomiting etc….

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14
Q

how can cyclosporin be administered?

A

parenteral, eyes, oral

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15
Q

how is azathioprine administered?

A

intravenous and orally

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16
Q

what drug class is clopidogrel?

A

a P2Y12 antagonist/ anti-platelet therapy agent

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17
Q

what is clopidogrel’s mechanism of action? What enzyme does it require?

A

it irreversibly blocks P2Y12 receptors and therefore blocks the binding site of ADP which is a platelet agonist and can act as a secondary agonist that is critical to complete platelet activation. this means the activation of GP11b/111a receptor is reduced leading to a reduction in fibrinogen binding and thrombus formation.
CYP450 enzymes to produce the active metabolite as its a prodrug.

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18
Q

what are the indications of clopidogrel?

A

prevention of atherothrombi events

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19
Q

what are the side effects of clopidogrel?

A

diarrhoea, GI discomfort, haemorrhage and skin reactions

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20
Q

how is clopidogrel administered?

A

orally

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21
Q

what drug class is heparin?

A

an anticoagulant agent

22
Q

how does heparin prevent the formation of fibrin?

A

heparin in combination with antithrombin2 can inhibit thrombosis by inactivating factor Xa and thrombin. Once active thrombosis has developed, larger amounts of heparin can inhibit further coagulation by inactivating thrombin and preventing the conversion of fibrinogen to fibrin.

23
Q

how does heparin prevent the formation of stable fibrin clots?

A

it inhibits the activation of the fibrin stabilising factor

24
Q

what are the indications of heparin?

A

pulmonary embolisms, arteriole occlusions, angina, deep vein thrombosis, thromboprophylaxis, haemodialysis, prevention of clotting

25
Q

what are the side effects of heparin?

A

haemorrhage, heparin-induced-thrombocytopenia, skin reactions, thrombocytosis

26
Q

how is heparin administered?

A

intravenously

27
Q

what drug class is lepirudin?

A

anti-thrombin agent/ anticoagulant

28
Q

what is the mechanism of action of lepirudin?

A

it forms a stable non-covalent complex with thrombin, preventing fibrinogen cleavage and initiation of the clotting cascade.

29
Q

lepirudin has been withdrawn. what has it been replaced with?

A

dabigatran or apixaban

30
Q

what is dabigatran?

A

a direct thrombin inhibitor

31
Q

what is apixaban?

A

a factor Xa inhibitor

32
Q

what are the indications for lepirudin?

A

heparin-induced thrombocytopenia (HIT) and associated thromboembolic disease

33
Q

what are the side effects of lepirudin?

A

sudden numbness or weakness (especially on one side of the body), sudden headache, confusion, problems with speech, or balance; bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds; red or pink urine

34
Q

how is lepirudin administered?

A

orally

35
Q

what drug class is prednisolone?

A

a glucocorticoid receptor agonist/cotricosteroid/ immunosuppressant

36
Q

what is prednisolone derived from? where is it metabolised?

A

it is derived from cortisone and is metabolised in the liver to prednisolone

37
Q

what is prednisolone’s mechanism of action?

A

prednisolone can cross cell membranes and bind to cortisone receptors. this leads to changes in DNA transcription, reducing the production of inflammatory proteins. it can also affect cell membrane ion permeability and neurohormone production.

38
Q

what are the indications for prednisolone?

A

COPD, croup, asthma, inflammation, allergic reactions, Crohn’s disease, myasthenia gravis etc…

39
Q

what are the side effects of prednisolone?

A

anxiety, abnormal behaviour, cognitive impairment, Cushing’s syndrome, electrolyte imbalance, fatigue, Gi discomfort, headache…

40
Q

how is prednisolone administered?

A

ear, eye, intra-articular, intramuscular and oral

41
Q

what drug class is tetanus booster?

A

vaccination therapy

42
Q

why must a tetanus booster be given?

A

to ensure a resistance to tetanus infection as we give an inactive tetanus which induces a weaker immune response

43
Q

what does an inactive vaccine contain?

A

virus/bacterial particles which are grown in the lab but have been killed using heat or formaldehyde.

44
Q

how can inactive vaccines be split into groups?

A

whole virus, split virus and subunit virus

45
Q

when should the booster be given?

A

every 10 years but it can be given within 2 days of the patient’s injury if needed

46
Q

what drug class is warfarin?

A

a vitamin K antagonist/ anticoagulant

47
Q

what is warfarin used to prevent?

A

thromboembolic diseases e.g. venous thrombosis, thromboembolism, pulmonary embolism and ischemic stroke

48
Q

why should you not take warfarin when pregnant?

A

as it can cross the placental barrier resulting in foetal bleeding, spontaneous abortions and neonatal death

49
Q

describe warfarin mechanism of action?

A

it inhibits vitamin K reductase, reducing levels of the reduced form of vitamin k which is require for the production of coagulation factors II, IIV, IX and X and anticoagulant proteins C and S. depression of these coagulation factors results in decreased prothrombin levels, decreased thrombin generation and reduced ability to form a clot

50
Q

what are the indications of warfarin?

A

Prophylaxis of embolisation in rheumatic heart disease, atrial fibrillation, after insertion of prosthetic heart valve, venous thrombosis and pulmonary embolism and
transient ischaemic attacks

51
Q

what are the side effects of warfarin?

A

alopecia, nausea, vomiting

52
Q

how is warfarin administered?

A

orally

B4W2 (11 decks)

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