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All Drugs Flashcards

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1
Q

Lisinopril/ramipril

A

Indication: hypertension and heart failure

Class: ACEi

Actions:

  • inhibit angiotensin I to angiotensin II
  • build up of bradykinin - vasodilation via NO

Adverse effects:

  • dry cough (bradykinin)
  • hyperkalaemia (low aldosterone)
  • cause/worsen renal failure (dont give renal artery stenosis)
  • angiodema (afro-carribean patients)

Warnings:

  • preganncy - may cause newborn hypotension via breastfeeding
  • dont give in low renin patients - loss of RAAS and become hypotensive
  • renal artery stenosis
  • afro-carribean

Interactions:

  • potassium increasing drugs (amiloride, ARBs)
  • NSAIDs
  • other antihypertensives

Other:

  • less effective than ARBs as angiotensin II produced from angiotensin I independently of ACE via chymases
  • used in hypertension with type II diabetes - decreases peripheral vascular resistance and dilates efferent arteriole so reduces glomerular pressure
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2
Q

Losartan

A

Inidication: hypertension and heart failure

Class: Angiotensin receptor II antagonist - AT1 receptor

Adverse effects:

  • hypotension
  • hyperkalaemia (low aldosterone)
  • cause/worsen renal failure (dont give w/ renal artery stenosis)

Interactions:

  • potassium increasing drugs (amiloride, ACEi)
  • NSAIDs

Warnings:

  • pregnancy
  • low renin patients - loss of RAAS so become hypotensive

Other:

  • more effective at inhibiting angiotensin II mediated vasoconstriction - block further down stream
  • no effect on bradykinin and angiodema less likely than with ACEi
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3
Q

Amlodipine/nimodipine

A

Indication: hypertension

Class: dihydropyridine calcium channel blocker

Action:

  • amlodipine selective for peripheral calcium initiated vascular smooth muscle contraction
  • nimodipine selective for cerebral vasculature - useful for ischaemic effects of subarachnoid haemorrhage

Adverse effects:

  • ankle swelling
  • flushing + headaches (vasodilation)
  • palpitations (compensatory tachycardia)

Contraindications:

  • unstable angina
  • severe aortic stenosis

Interactions:
- simvastatin (increases statin effect)

Other:

  • give instead of ACEi for low renin patients
  • amlodipine has long half life
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4
Q

Verapamil

A

Indication: arrythmia, angina

Class: phenylalkylamines - non dihyropyridine CCB

Actions: negative chronotropic and inotropic effects

Adverse effects:

  • constipation
  • bradycardia (dont give w/ AV nodal delay)
  • heart block and cardiac failure (dont give with poor LV function)

Interactions:

  • beta blockers
  • other antihypertensives and atiarrythmics
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5
Q

Indapamide

A

Indication: hypertension

Class: thiazide diuretic

Action:

  1. inhibit Na+/Cl- transporter in distal convoluted tubule - decrease Na+ and h20 reabsorption
  2. Long term - sensitivty of vascular smooth muscle to vasoconstrictors (calcium and noradrenaline)

Adverse effects:

  • hypokalaemia, hyponatreamia, hyperuricemia (gout)
  • increase glucose
  • increase cholesterol and triglyceride

Interactions:

  • NSAIDs
  • K+ decreasing drugs e.g loop diuretics

Other:

  • useful over calcium channel blockers in oedema
  • single dose in morning - causes you to urinate so could disrupt sleep if taken later in the day
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6
Q

Doxazosin/tamulosin

A

Indication: resistant hypertension

Class: alpha adrenoreceptor blocker

Action:

  • reduce peripheral vascular resistance
  • tamsulosin used in BPH - dilation of bladder neck and prostate

Adverse effects:
- postural hypotension, dizziness, syncope, headache

Interactions:
- dihydropyridine CCB - increase oedema

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7
Q

Labetalol/bisoprolol

A

Indication: resistant hypertension and heart failure

Class: beta blocker

Action:

  • decrease sympathetic tone by blocking NAd
  • reduce myocardial contraction, decreasing CO
  • decrease renin secretion - beta 1

Adverse effects:

  • bronchospasm (dont give w/ asthma)
  • heart block (dont give w/ Haemodynamic instability)
  • raynauds
  • mask tachycardia (insulin induced hypoglycaemia)

Interactions: non-dihydropyridine CCBs - overload

Other:

  • used in resistant hypertension
  • used in gestational diabetes and pregnancy hypertension
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8
Q

Spirinolactone

A

Indication: resistant hypertension and heart failure

Class: aldosterone receptor antagonist - block transcription (dont give w/ addisons)

Adverse effects:

  • hyperkalaemia
  • gynaecomastia (anti-androgen)

Interactions:

  • K+ increasing drugs
  • pregnancy
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9
Q

Furosemide

A

Indication: heart failure

Class: loop diuretic

Action: inhibit N+/K+/2Cl- in ascending LoH, decrease H20 absorption

Adverse effects:

  • dehydration and hypotension
  • hypokalamia, hyponaetreamia, hyperuricemia (gout)
  • tinnitus (ototoxicity)

Interactions:

  • aminoglycosides - ototoxicity
  • digoxin - hypokalaemia
  • lithium
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10
Q

Amiloride

A

Indication: heart failure

Class: potassium sparing diuretic

Action: directly block ENaC - decrease sodium reabsoprtion and decrease potassium excretion (dont give w/ addisons)

Adverse effects: hyperkalaemia

Interactions: other K+ sparing drugs (ACEi, ARBs)

Other:
- often used w/ loop or thiazide diuretics to decrease potassium loss

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11
Q

Atorvastatin/simvastatin

A

Indication: hyperlipidaemia

Class: statin

Action:

  • competitive inhibition of HMG- CoA reductase
  • upregulation of hepatic LDL receptors
  • increased clearance of circulating LDL

Adverse effects:

  • GI disruption, nausea, headache
  • myalgia
  • rhabdomylosis

Warnings:

  • renal/hepatic impairement
  • pregnancy and breastfeeding

Interactions:

  • amlodipine - increases plasma statin
  • amiodarone, macrolides - increase statin (CYP3A4 inhibtion)
  • grapefruit juice inhibits CYP3A4

Other:

  • simvastatin - prodrug activated by FPM - short half life
  • atorvastatin - FPM produces further active metabolites - long half life
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12
Q

Fenofibrate

A

Indication: hyperlipideamia

Class: fibric acid derivatives

Action: activation of nuclear transcription factor PPARa - increase production of lipoprotein lipase

  • increase triglyceride removal from lipoprotein in plasma
  • increase fatty acid uptake by liver
  • increase levels of HDL
  • increase LDL affinity for receptor

Adverse effects:

  • gall stones (avoid w/ gall bladder disease)
  • GI upset
  • myositis
  • photosensitivity

Interactions: warfarin - increase anticoagulation

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13
Q

Ezetimibe

A

Indication: hyperlipideamia

Class: cholesterol absoprtion inhibitors

Action:

  • inhibit NPC1L1 transporter at brush border in SI
  • redcues absorption of cholesterol by gut
  • increase expression of hepatic LDL receptor
  • prodrug, hepatic metabolism, enterohepatic circulation, limits systemic exposure, secreted by bile

Adverse effects:

  • abdo pain, GI upset
  • angioedema

Warning: hepatic failure - pro drug so part of hepatic metabolism and enterohepatic circulation

Interactions:

  • mindful with statin - increased risk of rhabdomyloysis
  • ciclosporin - increases ezetimibe

Other: adjunct to statin

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14
Q

Alirocumab

A

Indication: hyperlipideamia

Class: monoclonal antibody

Action: PCSK9 inhibitor - prevent protein binding to internalised LDL-R, prevent degradation, decrease blood levels of LDL cholesterol

Adverse effects:

  • long term effects unknown
  • requires lifetime injections
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15
Q

Inclisiran

A

Indication: hyperlipideamia

Class: siRNA

Actions: inhibits hepatic translation of PCSK9 so less produced, less binding to internalised LDL-R, less degradation, less blood LDL-C level

Adverse effects:

  • long term effects unknown
  • requires lifetime injections
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16
Q

Oestrogen

  • actions
  • side effects
A

Actions:

  • mild anabolic
  • sodium and water retention
  • raises HDL, lowers LDL
  • decrease bone resorption
  • impaired glucose tolerance
  • increase blood coaguability

Side effects:

  • water retention
  • nausea, vomiting
  • thromboembolism
  • imapaired glucose tolerance
  • increase blood coaguability
  • breast tenderness
  • endometrial + breast hyperplasia and cancer
  • ovarian metaplasia and cancer
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17
Q

Progesterone

  • actions
  • side effects
A

Actions:

  • anabolic
  • fluid retention
  • increase bone mineral density
  • secreteroy endometrium
  • mood changes
  • maintains pregnancy

Side effects:

  • anabolic
  • fluid retention
  • nausea/vomiting
  • acne
  • weight gain
  • irritability, depression, PMS
  • lack of concentration
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18
Q

Testosterone

- actions/side effects

A
  • anabolic
  • male secondary sexual characterstics
  • acne
  • voice changes
  • agression
  • decrease HDL-C/LDL-C (increase atherosclerotic risk)
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19
Q

Alendronic acid

A

Indication: osteoporosis, pagets disease, malignancy

Class: bisphosphonates

Actions: control osteoclast activity - reduce bone turnover

Adverse effects:

  • oesophagitis (remain upright for 30 mins after)
  • hypocalcaemia (check ca and vit D levels before)

Other:

  • long half life
  • poor gut absoprtion
  • absoprtion affected by food - empty stomach
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20
Q

Mifepristone

A

Indication: termination of pregnancy

Class: progesterone (and glucocorticoid) receptor antagonist

Actions: sensitises the myometrium to prostaglandin-induced contracions

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21
Q

Finasteride

A

Indication: BPH

Class: 5-alpha reductase inhibitor

Actions: prevent conversion of testosterone to dihydrotestosterone

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22
Q

Clomiphene

A

Indication: anovulation

Class: SERM

Action:

  • competes with oestrogen for ER binding
  • increased production of anterior pituitary hormones
  • leads to ovulation induction
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23
Q

Raloxifene

A

Indication: osteoporosis

Class: SERM

Action: bone specific

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24
Q

Tamoxifen

A

Indication: breast cancer

Class: SERM

Action:

  • active metabolites compete with oestrogen for binding to the ER
  • causes cells to arrest in the cell cycle

Adverse effects: in endometrium acts as an ER agonist - increased risk of endometrial hyperplasia/cancer

Other:

  • pro drug therefore metabolised in the liver to active derivatives
  • genetic differences in enzymes in the liver means tamoxifen is not metbaolised and therefore not active in some people
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25
Q

Ulipristal acetate

A

Indication: emergency contraception, uterine fibroids

Class: SPRM

Action: delay/inhibit ovulation

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26
Q

Insulin

A

Indication: type 1 diabetic/ late stage type 2

Adverse effects:

  • hypoglycaemia
  • lipodystophy (rotate site of administration)

Warning: renal impairement - hypoglycaemia risk

Interactions:

  • systemic steroids - need to increase insulin dose
  • other hypoglycaemic agents

Other:

  • protein so must be given paraenterally to avoid digestion
  • short half life so slow absoprtiom via soluble insulin or insulin analogues
27
Q

Metformin

A

Indication: hyperglycaemia

Class: biguanides

Hypoglycaemia: no

Weight: supress apetite

Route: oral

Action: reduces hepatic glucose by inhibiting gluconeogenesis

Adverse effects: GI upset - nausea, vomiting, diarrhoea

Warnings:

  • stop if eGFR <30 - excreted unchanged by the kidneys so can quickly accumulate
  • alcohol intoxication

Interactions:

  • ACEi, NSAIDs, diuretics - may impair renal function
  • loop and thiazide can increase glucose so reduce metformin action
28
Q

Gliclazide

A

Indication: hyperglyceamia

Class: sulfonylureas

Hypoglycaemia: yes

Weight: increased - anabolic effecrs of insulin

Route: oral

Action: stimulate pancreatic insulin secretion by blocking ATP-dependant K+ channels

Adverse effects: GI upset

Warnings: hepatic and renal disease

Interactions:

  • other hypoglycaemic agents
  • loop and thiazide can increase glucose so reduce SU action
29
Q

Pioglitazone/rosiglitazone

A

Indication: hypergylycaemia

Class: glitazone

Hypoglycaemia: yes

Weight: increased - fat cell differentiation

Route: oral

Action: enhanced insulin sensitivty and utilisation

Adverse effects:

  • GI upset
  • fluid retention
  • fracture risk
  • bladder cancer

Warnings: heart failure because of fluid retention

Interactions: other hypoglycaemic agents

30
Q

Dapagliflozin/canagliflozin

A

Indication: hyperglycaemia

Class: SGLT-2 inhibitors

Hypoglycaemia: no

Weight: decrease

Route: oral

Actions: reduce glucose reabsorption

Adverse effects:

  • UTI
  • genital infection
  • thirst and polyuria

Warnings: hypovolaemia - possible hypotension due to osmotic diuresis

Interactions: antihypertensives and other hypoglycaemic agents

31
Q

Sitagliptin/saxagliptin

A

Indication: hyperglycaemia

Class: DPP-4 inhibitor

Hypoglycaemia: no

Weight: reduce apetite

Route: oral

Action: prevent incretin degradation - promote insulin secretion and supress glucagon release

Adverse effects:

  • GI upset
  • pancreatitis

Warnings:

  • pregnancy
  • pancreatitis

Interactions:

  • other hypoglycaemic agents
  • drugs which increase glucose oppose gliptin action e.g thiazides
32
Q

Exenatide/liraglutide

A

Indication: hyperglycaemia

Class: GLP-1 receptor agonist

Hypoglycaemia: no

Weight: increased satiety

Route: SUBCUTANEOUS

Actions: increase glucose dependent synthesis of insulin

Adverse effects:

  • GI upset
  • decreased apetite with weight loss

Warnings: renal impairment

Interactions: other hypoglycaemic agents

33
Q

Aspirin

A

Indication: antiplatelet

  • AF patients post stroke
  • secondary prevention of stroke, TIA, ACS
  • post PCI to reduce ischaemic complications

Class: cyclo-oxygenase inhibitor

Action: low doses inhibits COX-1 mediated production of thromboxane A2 whcih reduces platelet aggregation - irreversible

Adverse effects:

  • GI irritation + bleeding (Peptic ulcer)
  • haemorrhage (stroke)
  • hypersensitivity

Warnings:

  • <16yrs - reye’s syndrome
  • 3rd trimester - premature closure of the ductus arteriosus
  • hypersensitivty

Interactions: other antiplatelets and anticoagulants

Other:

  • does not completely inhibit platelet aggregation due to other endodgenous pathways
  • absorbed by passive diffusion - hepatic hydrolysis to salicylic acid
  • COX1 polymorphisms result in lack of efficacy in some
  • lasts lifespan of the platlet (7-10 days) - non nucleated therefore unable to produce more of COX1
  • gastric protection (PPI) required for long term use in at risk patients
34
Q

Clopidogrel/prasugrel/ticagrelor

A

Indication: dual antiplatlet therapy

  • ischaemic stroke and TIA
  • long term monotherapy where aspirin in contraindicated

Class: ADP receptor antagonists

Actions: inhibit binding of ADP to P2Y12 receptor therefore inhibits activation of GPIIb/IIIa receptors (independent of COX pathway)

Adverse effects:

  • bleeding
  • GI upset (dyspepsia and diarrhoea)
  • trombocytopenia

Warning: high bleed risk patients with renal and hepatic impairment

Interactions:

  • CYP inhibitors - omeprazole, ciprofloxacin, erythromycin, SSRIs (clopidogrel requires CYPs for activation)
  • tricagrelor can interact with CYP inhibitors and inducers
  • other antiplatelts, anticoagulants + NSAIDs - increase risk of bleeding

Other:

  • clopidogrel/prasugrel are irreversible inhibitors of P2Y12
  • ticagrelor acts reversibly at different site
  • clopidogrel/prasugrel are prodrugs - active hepatic metabolites
  • ticagrelor has active metabolites
  • most cases stopped 7 days prior to surgery
35
Q

Dipyridamole

A

Indication: antiplatelet

  • secondary prevention of ischaemic stroke and TIA
  • adjunct for prophylaxis of thromboembolism following valve replacement

Class: phosphodiesterase inhibitor

Action:

  1. inhibits cellular reuptake of adenosine - increased adenosine inhibits platelet aggregation via A2 receptors
  2. PDE inhibitor - prevents cAMP degradation therefore inhibits expression of GPIIb/IIIa

Adverse effects: V+D, dizziness

Interactions: antiplatelets, anticoagulants, adenosine

36
Q

Abciximab

A

Indication: antiplatelet
- specialist use in high risk percutaneous transluminal coronary angioplasty

Class: GP IIb/IIIa inhibitor

Action: blocks binding of fibrinogen and vWF - targets final common pathway therefore more complete reduction in aggregation (>80%) - i.v

Adverse effect: bleeding - dose adjusted for body weight

Interactions: other antiplatlets and anticoagulants

37
Q

Streptokinase/alteplase

A

Indication: fibrinolytic

Action: inhibit plasminogen to plasmin therefore inhibits degradation of fibrin clot

Adverse effects: bleeding

Interactions: antiplatelets and anticoagulants

Other:

  • alteplase (tPA) in acute ischaemic stroke
  • streptokinase following STEMI
  • streptokinase can only be used once - antibodies develop as it is derived from bacteria
38
Q

Lidocaine/mexiletine

A

Indication: arrythmias
- ventricular tachycardia

Class: Ib

Action:

  • fast binding offset kinetics
  • blocks the open/inactive Na+ channels (fast beating/ischaemic tissue)
  • decrease phase 0 depolarisation - decrease conduction velocity in ischaemic tissue

ECG: prolong QRS

Side effects:

  • CNS: dizziness, drowsiness
  • abdominal upset

Route:

  • lidocaine iv only
  • mexiletine oral only
39
Q

Flecainide

A

Indication: arrythmias

  • supraventricular arrythmias
  • premature ventricular contrcations
  • wolff-parkinson-white syndrome

Class: 1c

Action:

  • very slow binding offset kinetics
  • block open/inactivated Na+ channels - slow phase 0 in normal tissue
  • increase threshold, decrease automaticity
  • increase APD and refractory period in rapdily depolarizing atrial tissue

ECG: increase PR, QRS, QT

Side effects:

  • pro-arrythmia and sudden death especially with chronic use
  • felcainide flutter - increase ventriuclar response to supraventricular arythmias
  • CNS and GI effects (local anesthetics)

Route: oral or iv

40
Q

Propanolol/bisoprolol/metoprolol/esmolol

A

Indiction: arrythmias

  • tachycardia
  • re-entry arryhthmias
  • atrial fibrilation - slow AVN conduction, protect ventricles
  • CAN give in stable heart failure, NOT in partial AV block or acute heart failure

Class: II

Actions:

  • act at beta 1 receptors in the heart (block sympathetic effect)
  • pacemaker cells = decrease phase 4 depolarization, decrease AVN conduction velocity
  • non pacemaker cells = increase APD and refractory period

ECG: increase PR, decrease HR

Side effects:

  • bronchospasm - non selective beta2 receptors in the lungs
  • hypotension

Route:

  • propanolol/metoprolol = oral or iv
  • bioprolol = oral
  • esmolol = iv only (very short acting/half life)
41
Q

Amiodarone

A

Indication: arrythmias

Class: III

Action:
Non pacemaker cells=
- K+ block - increase APD and refractory period
- Na+ block - decrease phase 0, decrease conduction

Pacemaker cells =
- beta and Ca+ block - decrease phase 4 depolarisation, decrease AVN conduction

ECG: increase PR, QRS, QT, decrease HR

Side effects:

  • pulmonary fibrosis
  • hepatic injury
  • increase LDL cholesterol
  • thryoid disease
  • photosensitivty
  • optic neuritis
  • reduce dose of digoxin and monitor warfarin more closely

Route: oral or iv

42
Q

Sotalol

A

Indication: arrythmias
- supraventricular and ventircular tachycardia

Class: III

Action:

  • K+ block - increase APD and refractory period
  • beta blocker - decrease phase 4 depolarisation, decrease AVN conduction

ECG: increase QT, decrease HR

Side effects:

  • proarrythmia
  • fatigue and insomnia

Route: oral

43
Q

Verapamil/diltiazem

A

Indication: arrythmias
- supraventricular tachycardia - control ventricles and convert to normal sinus rhythm (re-entry around AVN)

Class: IV

Action:

  • Ca+ channel blocker
  • decrease phase 0, decrease conduction through AVN
  • increase refractory period in AVN
  • negative chronotropic and inotropic effects

ECG:

  • increase PR
  • increase/decrease HR - depends on BP response and baroreflex

Side effects:

  • hypotension, decreased CO, sick sinus
  • asystole - if partial AV block and beta blocker present
  • GI problems - constipation

Route:

  • verpamil = oral or iv
  • diltiazem = oral
44
Q

Adenosine

A

Indication: arrythmias

  • convert re-entrant supraventricular arrythmias
  • diagnosis of coronary artery disease (compare perfusion of the heart when beating slowly vs fast)

Class: V

Action:

  • binds to a1 receptors and blocks adenyl cyclase - reduce cAMP
  • decrease Ca+, increase refractory period, slow AV conduction
  • activation of K+ currents in SAN/AVN - hyperpolarisation - decrease HR

Route: rapid iv bolus (very short half life)

45
Q

Ivabradine

A

Indication: arrythmias

  • sinus tachycardia
  • reduce HR in heart failure and angina

Action:

  • blocks funny current in SAN
  • slows SAN
  • DOESN’T effect blood pressure

Side effects:

  • flashing lights
  • avoid in pregnancy

Route: oral

46
Q

Digoxin

A

Indication: arrythmias
- heart failure with arryhtmia present

Class: cardiac glycoside

Action:

  • enhances vagal activity - slows AV conduction and HR
  • block Na+/K+ ATPase, increase intracellular Na+, decrease activity of NCX, increase intracellular Ca+, increase force of contraction

Side effects: v dependent on renal function - decrease function can increase blood levels and cause extreme bradycardia

47
Q

Atropine

A

Indication: arrythmias
- treat vagal bradycardia e.g fainting

Action:

  • selective muscarinic anatgonist
  • block vagal activity - increase AV conduction and HR
48
Q

Corticosteroids

A

Indication: immunosuppressant

Action:

  • Prevent IL-1 and IL-6 production by macrophages
  • inhibit all stages of T cell activation
49
Q

Azathioprine

A

Indication: immunosuppresant

  • MAINTENANCE therapy for SLE and vasculitis
  • IBS
  • atopic dermatitis, bullous skin disease
  • steroid sparing drug

Action:

  • cleaved to 6-MP
  • metabolised by TPMT to TIMP
  • anti-metabolite decreases DNA and RNA synthesis (purine)

Adverse effects:

  • bone marrow supression - monitor FBC
  • increased risk of malignancy - especially transplanted patients
  • increased risk of infection
  • hepatitis - monitor LFT

Other: TPMT gene highly polymoprhic so test activity before prescribing (low/absent levels = risk of myelosupression)

50
Q

Ciclosporin/tacrolimus

A

Indication: immunosupressant

  • transplantation
  • atopic dermatitis and psoriasis
  • not often rheumatology - renal toxicity - check BP and eGFR

Class: calcineurin inhibitor

Action:

  • ciclosprin binds to cyclophilin protein
  • tacrolimus binds to tacrolimus-binding protein
  • drug/protein complexes bind to calcineurin
  • inhibit calcineurin, prevent production of IL-2 from T helper cells

Adverse effects:

  • bone marrow supression - monitor FBC
  • increased risk of malignancy - especially transplanted patients
  • increased risk of infection
  • hepatitis - monitor LFT

Other: inhibit CYP 450 - multiple drug intercations possible

51
Q

Mycophenolate mofetil

A

Indication: immunosupressant

  • transplants
  • INDUCTION and MAINTENANCE in lupus nephritis
  • MAINTENANCE in vascultitis

Action:

  • prodrug derived from fungus penicllium stoloniferum
  • inhibits inosine monophosphate dehydrogenase (guanosine synthesis)
  • impairs B and T cell proliferation
  • spares other rapidly diving cells - guanosine salvage pathways

Adverse effects:

  • nausea, vomiting, diarrhea
  • myelosupression
52
Q

Cyclophosphamide

A

Indication: immunosupression

  • lymphoma, leuakemia, solid cancers
  • lupus nephritis
  • wegener’s granulomatosis

Actions:

  • prodrug - active metabolites are 4-hydroxycylcophosphamide and its tautomer aldophosphamide
  • alkylating agents - cross link DNA so that it cannot replicate and supress B and T cell activity
  • aldophosphamide converted to carboxyphosphamide (inactive), phosphoramide mustard (good metabolite), acrolein (toxic metabolite to the bladder leading to hemorrhagic cystitis - prevented by aggressive hydration and mesna)

Adverse effects: toxicity

  • increased risk of badder cancer, lymphoma and leukaemia
  • infertility (risk relates to cumulative dose and pateint age)
  • monitor FBC and adjust dose in renal impairment

Other:
- mycophenolate mofetil safer and as effective in lupus nephritis

53
Q

Methotrexate

A

Indication: immunosuppressant

  • gold standard for RA
  • malignancy
  • psoriasis
  • crohn’s
  • abortions

Action:

  1. Malignant disease:
    - competitively and reversibly inhibits dihydrofolate reductase
    - inhibits conversion of dihydrofolate to active tetrahydrofolate (key in purine and thymidine synthesis)
    - inhibits synthesis of DNA, RNA and proteins - cytotoxic effect during S phase therefore more effective on rapdily dividing cells
  2. Non malignant disease:
    - unclear
    - NOT via anti-folate action
    - possibly inhibition of accumulationof adenosine

Route: oral, IM or SC (if only partial response or nausea)

Dosing: WEEKLY - long half life

Adverse effects:

  • mucositis (responds to folic acid supplementation)
  • marrow supression (responds to folic acid supplementation)
  • hepatitis/cirrhosis
  • pneumontis
  • infection
  • highly tetratoegnic and abortifacient

Other:

  • 50% protein bound - NSAIDS displace
  • renal excretion
54
Q

Sulfasalazine

A

Indication: immunosupressant

  • IBD (poorly absorbed - main activity in the intestine)
  • RA

Action:

  • 5-ASA anti-inflamatory, sulfapyridine antibiotic
  • T cell inhibtion of proliferation and IL-2 production, apoptosis
  • neutrophil - reduce chemotaxis and degranulation

Adverse effects:

  • myelosuppression
  • hepatitis
  • rash
  • nausea, vomiting, abdo pain

Other:

  • safe in pregnancy
  • few drug interactions
  • effective and favourable toxicity
55
Q

Adalimumab, infliximab

A

Indication: immunosupressant

  • RA
  • IBD
  • psoriasis
  • psoriatic arthritis
  • ankylosing spondilitis

Class: monoclonal antibody

Action: blocks/binds TNFa

  • decrease inflamation - cytokine cascade, leukocutes to joint
  • decrease angiogenesis - VEGF levels
  • decrease joint destruction - MMps, bone reorption/erosion, cartilage breakdown

Adverse effects: TB reactivation - TNFa released by macrophages in response to TB infection and is essential for development and maintenenace of granulomata (screen for latent TB before anti-TNF treatement)

56
Q

Rituximab

A

Indication: immunosupressant

  • RA
  • vasculitis
  • systemic lupus erythramotosus
  • lymphoma

Class: monoclonal antibody

Action:

  • binds to CD20 found on a specific subset of B cells (not stem or plasma cells)
  • causes B cell apoptosis (loss of antigen presentation to T cells, cytokines, antibodies)
57
Q

Aspirin, ibuprofen, naproxen

A

Indication: anti-inflamatory, analgesia, antipyretic

  • inflammatory conditions
  • oestoarthritis
  • post operative pain
  • menorrhagia
  • low dose asprin for platelt aggregation (COX1)

Class: NSAIDs

Action:
- inhibit COX1 - decrease prostaglandins, prostacylcin, thromboxane synthesis

Adverse effects:

  • GI - dyspepsia, nausea, ulceration, bleeding (PGE2 regulates acid secretion in parietal cells, PGI2 maintains blood flow and mucosal repair)
  • renal - reversible decreased GFR and renal blood flow (PGE2/PGI2 vasodilation of afferent arteriole), increased blood pressure (PGE2 inhibits sodium absoprtion in the collecting duct)

Warnings:

  • GI - IBD, elderly, prolonged use, smoking, alcohol, H.pylori, ulcers
  • renal - CKD, heart failure (greater reliance on PGE2 for vasodilation)
  • pregnancy - delayed labour and early closure of ductus arterosus

Interactions:

  • GI - aspirin, glucocorticoid steroids, anticoagulants (PPI considered)
  • renal - ACEi, ARbs, diuretics

Other:
- displace other highly protein bound drugs (sulfonylurea + hypoglycaemia, methotrexate + haeptoxicity, warfarin + increaed bleed risk)

58
Q

celecoxib, etoricoxib

A

Indication: antiinflammatroy, analgesic, antipyretic
- long term osteo/rheumatoid arthritis

Class: NSAID

Action: selective COX2 inhibitors

Adverse effects:

  • less gi
  • renal - CKD, heart failure (greater reliance on PGE2 for vasodilation)
  • increase MI risk - inhibit PGI2 - unopposed aggregatory effects
59
Q

Paracetemol

A

Indication: analgesic and antipyretic

Action: COX2 selective inhibtion in CNS - decrease pain signals to higher centres (little anti-inflmatory action as peroxides in peripheral inflamation)

Adverse effects:

  • few ADRs
  • no effect on platelets
  • limited effect on GI
  • well abrobed from GI - inactivated by conjugation in liver

Overdose:

  • at normal doses conjugation with glutathione renders NAPQI harmless
  • hepatic glutathione is limited
  • NAPQI highly nucleophilic - oxidises key enzymes causing necrosis and apoptosis
  • asymtomatic initially, nausea + vomiting in 24hr, liver damage 3-4days
  • iv acetylcysteine - glutathione thiol replacement (glutathione itself cannot get into hepatocytes)
60
Q

Morphine

A

Indication: opioid
- analgesic

Class: opioid agonist (strong)

Action:

  • binds to MOP receptor
  • decrease cAMP
  • efflux of potassium - hyperpolarisation
  • decrease substance P and GABA release
  • increase dopamine release

Absorption:

  • PO, IV, IM, SC, PR
  • erratic gut absorption
  • FPM - 40% oral bioavilability

Distribution:

  • very lipophilic - enters all tissues (including foetal)
  • not protien binding so struggles to cross BBB

Adverse effects:

  • respiratory depression -decreases sensitivity of MRC to CO2
  • GI tract - constipation, vomiting
  • CVS
  • miosis
  • histamine release - caution in asthmatics

Other:

  • metabolism = morphine + glucoronic acid = M6G + M3G
  • elimination = renal
61
Q

Fentanyl

A

Indication: opioid

  • analgesic
  • anasethetic

Class: opioid agonist (stronger)

Action:

  • binds to MOP receptor
  • decrease cAMP
  • efflux of potassium - hyperpolarisation
  • decrease substance P and GABA release
  • increase dopamine release

Absorption:

  • IV, epidural, inrathecal, nasal
  • 80- 100% oral bioavilability
  • 100x more potent and higher affinity than morphine

Distribution:

  • very lipophilic - enters all tissues (including foetal)
  • high protien binding so crosses BBB

Adverse effects:

  • respiratory depression -decreases sensitivity of MRC to CO2
  • GI tract - constipation, vomiting
  • histamine release - caution in asthmatics
  • LESS than morphine

Other:

  • metabolism = hepatic via CYP3A4
  • elimination = renal
62
Q

Codeine

A

Indication: opioid

  • analgesic
  • cough depressant

Class: opioid agonist (moderate)

Metabolism:

  • codeine to morphine via CYP2D6 (inhibited by fluoxetine)
  • variable expression of CYP = variable response
  • 1/10th potency of morphine

Action:

  • binds to MOP receptor
  • decrease cAMP
  • efflux of potassium - hyperpolarisation
  • decrease substance P and GABA release
  • increase dopamine release

Absorption:
- PO, SC

Adverse effects:

  • respiratory depression - worse in children
  • GI tract - constipation

Other:
- elimination = glucoronidation and renal excrection

63
Q

Buprenorphine

A

Indication: opioid

  • analgesic
  • addiction

Class: opioid partial agonist

Action:

  • binds to MOP receptor - low kd (high affinity), low Emax (effiacy)
  • decrease cAMP
  • efflux of potassium - hyperpolarisation
  • decrease substance P and GABA release
  • increase dopamine release
  • antagonist at KOP receptor

Absorption:
- transdermal, buccal, sublingual

Distribution:
- very lipophilic - enters all tissues (including foetal)

Adverse effects:

  • respiratory depression -decreases sensitivity of MRC to CO2
  • low bp, dizziness
  • nausea

Other:

  • metabolism = hepatic via CYP3A4
  • elimination = biliary excretion
64
Q

Naloxone

A

Indication: opioid

Class: competitive opioid antagonist

Action:

  • greater affinity for MOP than morphine, less than buprenorphine
  • inhibits normal cascade
  • 0 Emax

Absorption:

  • IV, IM, intranasal, PO
  • FPM - v low oral availability
  • rapid onset of action

Distribution:
- very lipophilic - enters all tissues (including foetal)

Adverse effects:

  • short half life
  • slow infusion

Other:

  • metabolism = hepatic - naloxone -3 - glucuronide
  • elimination = renal

CPT Drugs (16 decks)

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