50 Drugs Flashcards
Aspirin
Mechanism
- irreversible inactivation of COX enzyme
- reduces TXA2 production and endothelial prostaglandin (PGI2) production (reduces nociceptive sensitisation and inflammation)
GIVEN
after a thrombotic event
pain relief
SIDE EFFECTS:
bleeding
peptic ulceration
angioedema
clopidogrel
MECHANISM
- Irreversibly blocks the ADP-receptor on platelet cell membranes
- Consequently inhibits formation of GPIIb/IIIa complex, required for platelet aggregation.
GIVEN
secondary prevention of thrombotic events
SIDE EFFECTS
Bleeding
abdo pain
rtPA
Tenecteplase
Alteplase
MECHANISM
- Recombinant form of tissue plasminogen activator
- Catalyses conversion of plasminogen to plasmin
- Promotes fibrin clot lysis
GIVEN:
Ichaemic stoke LESS THAN 4.5 HOURS
MI within 12 hours
massive PE
SIDE EFFECTS
Bleeding
allergic reactions
unfractionated heparin AND LMWH
MECHANISM
- Enhances activity of antithrombin III.
- Antithrombin III inhibits thrombin.
- Heparins also inhibit multiple other factors of the coagulation cascade.
- This produces its anticoagulant effect.
GIVEN:
treatment and prophylaxis of thromboembolic disease (with VIT K antagonists)
- renal dialysis
- acute coronary syndrome
SIDE EFFECTS
- Bleeding
- heparin induce thrombocytopenia
- osteoporosis
Vit K antagonist - warfarin- give vitamin k to reverse the effects
Mechanism:
Inhibits vitamin K epoxide reductase.
Prevents recycling of vitamin K to reduced form after carboxylation of coagulation factors II, VII, IX and X.
Prevents thrombus formation.
GIVEN:
- treatment of venous thromboembolism
- Thromboprophylaxis in: AF / metallic heart valves / cardiomyopathy
SIDE EFFECTS:
- Bleeding
- warfarin necrosis
- osteoporosis
dabigatran
Mechanism:
- Direct thrombin inhibitor; prevents conversion of fibrinogen to fibrin.
This prevents thrombus formation.
GIVEN:
- prophylaxis of venothromboembolism
SIDE EFFECTS:
bleeding and dyspepsia
Rivaroxaban and Apixaban
10 a antagonist
Inhibits conversion of prothrombin to thrombin, reducing concentrations of thrombin in the blood.
prevents formation of fibrin clots
GIVEN:
prophylaxis of VTE
and treatment
SIDE EFFECTS:
bleeding and nausea
bisoprolol and atenolol
cardioselective beta blockers
Preferentially blocks beta-1 receptors in cardiac and renal tissue.
Inhibits sympathetic stimulation of the heart and renal vasculature.
GIVEN:
- Hypertension
- Angina
- Rate-control in atrial fibrillation
SIDE EFFECTS:
- Bradycardia
- hypotension
- bronchospasm
- cold extremities and sleep disturbances
propanolol and carvedilol
non-cardioselective beta blockers
GIVEN
Hypertension
Angina
Anxiety
Migraine prophylaxis
SIDE EFFECTS:
- Bradycardia
- hypotension
- bronchospasm
- cold extremities and sleep disturbances
Ramipril
Enalapril
Lisinopril
Perindopril
ACE INHIBITORS
Inhibits conversion of Angiotensin I to Angiotensin II (a more potent systemic vasoconstrictor)
GIVEN
Hypertension
Heart Failure
Nephropathy
Prevention of Cardiovascular events in high risk patients
SIDE EFFECTS
Dry cough (10% of Patients, causing cessation of treatment in 5%)
Hypotension
Hyperkalaemia
Renal Impairment
Angioedema
nitrates
GTN and isosorbide
mechanism:
- converted to NO which is a potent vasodilator
- cardioselective and act predominantly on coronary blood vessels which enhance blood flow to the ischaemic areas of the myocardium and reduces preload and after load
GIVEN:
- angina
- severe hypertension
side effects:
- headache
- postural hypotension
- tachycardia
verapamil and diltiazem
these are rate limiting calcium channel blocker drugs
mechanism:
- block the cellular entry of calcium by blocking l-type calcium channels
- decrease contraction of myocardial and smooth muscle
- prolong the AV node conduction which depresses the heart rate
GIVEN:
- supra ventricular arrthymias
- treatment of angina
- hypertension
side effects:
- constipation
ankle swelling in diltazem
- flushing
amlodipine
nifedipine
felodipine
NON-rate limiting calcium channel blockers
mechanism:
- block the cellular entry of calcium by blocking l-type calcium channels
- decrease contraction of myocardial and smooth muscle
GIVEN:
- treatment of angina
- hypertension
side effects:
- ankle oedema
- abdo pain
simvastatin
atorvastatin
pravastatin
HMG CoA reductase inhibitors
increases the amount of LDL-receptor expression on hepatocytes which increases the level of uptake of cholesterol
GIVEN:
- familial hypercholesterolaemia
- prevent of cardiovascular disease evens in high risk patients
side effects:
- myalgia
- GI disturbances
simvastatin
atorvastatin
pravastatin
HMG CoA reductase inhibitors
increases the amount of LDL-receptor expression on hepatocytes which increases the level of uptake of cholesterol
GIVEN:
- familial hypercholesterolaemia
- prevent of cardiovascular disease evens in high risk patients
side effects:
- myalgia
- GI disturbances
digoxin
cardiac glycosides
mechanism:
- Increases vagal parasympathetic activity and inhibits the Na+/K+ pump, causing a buildup of Na+ intracellularly.
in an effort to remove this build up of sodium, more calcium is brought into the cells by the exchangers
this build up means there is an increased force of contraction and reduced rate of conduction through the AV node
GIVEN:
- heart failure
- rate control in AF
side effects:
- nausea
- vomiting
- diarrhoea
- confusion
amiodarone
anti-arhythmic drug which blocks cardiac potassium channels and therefore prolong repolarisation of the cardiac action potential
GIVEN:
- supraventrivular and ventricular arthymias
side effects:
- photosensitivity skin reactions
- hypersensitivity reactions
Flucloxacillin
Amoxicillin
Benzylpenicillin
Penicillin V
beta-lactams
mechanism:
Attaches to penicillin-binding-proteins on forming bacterial cell walls.
This inhibits the transpeptidase enzyme which cross-links the bacterial cell wall.
Failure to cross-link induces bacterial cell autolysis.
indication:
fluclox use in skin infections
amox in non severe community acquired pneumonia
side effects:
- rash
- diarrhoea
ceftriaxone
cephalexin
cephalosporins
GIVEN:
Serious infection: septicaemia / pneumonia / meningitis
side effects:
- hypersensitivity
- c.diff
- liver function impairment
vancomycin
glycopeptides
bactericidal and inhibit cell-wall synthesis on gram positive bacteria
given:
- severe gram postiive infections
- MRSA
- severe c.diff
side effects:
- fever
- rash
gentamicin
aminoglycoside
mechanism:
binds to 30s ribosomal subunit which inhibits protein synthesis which induces a prolonged post-antibiotic effect
GIVEN:
- severe gram -ve infections and some soft tissue infections if gram positive
side effects:
- nephrotoxicity
- ototoxicmy
ciprofloxacin
quinolones
mechanism:
infers with bacterial DNA replication and repair
broad spectrum bactericidal antibiotics, provides both +ve and -ve cover
GIVEN:
Gram negative bacterial infection
Respiratory tract infection
Upper urinary tract infection
Peritoneal infection
Gonorrhoea
Prostatitis
SIDE EFFECTS:
GI toxicity
QT wave prolongation
C.diff
tendonitis
clarithromycin and erthromycin
macrolides
binds to 50s ribosomal subunit and inhibits bacterial protein synthesis IS BACTERIOSTATIC AND BACTERIOCIDAL
GIVEN:
Atypical organisms causing pneumonia / Severe community acquired pneumonia
Severe campylobacter infection
Mild / moderate skin and soft-tissue infection
Otitis media
Lyme disease
Helicobacter pylori eradication therapy
SIDE EFFECTS:
diarrhoea
vomiting
QT wave prolongation
ototoxicity with long term use
trimethoprim
inhibitor of folate synthesis
interferes with bacterial DNA replication
GIVEN:
First line antibiotic in uncomplicated UTI.
Acute / chronic bronchitis
Pneumocystis pneumonia (PCP)
Good range of action against gram negative and gram positive bacteria. Including some MRSA cover.
side effects:
elevated serum creatinine
hyperkalaemia
depressed haemotapoesis
rash and GI disturbances
acyclovir
anti-viral
a guanosine derivative, converted to triphosphate by infected host cells and this then inhibits DNA polymerase, terminating the nucleotide chain nd inhabiting viral DNA replication
GIVEN:
Herpes simplex infection
Varicella zoster infection
side effects:
nausea
vomiting
local inflammation at the infusion site
salbutamol
beta-adrenergic bronchodilator
short acting beta 2 adrenoceptor agonist which relaxes bronchial smooth muscle inducing bronchodilaton
inhibit pro-inflammatory cytokine release from mast cells and TNF alpha release from monocytes which reduces airway inflammation
increase mucus clearance
given:
COPD
asthma
side effects:
tremor
tachycardia
headache
sleep disturbances
salmeterol
Beta-Adrenergic Bronchodilators
LONG ACTING
beclomethasone
inhaled corticosteroid
- anti-inflammatory effect on the airways and decreases the formation of pro-inflammatory cytokines
- upregulates beta-2 adrenoreceptors in the airways
GIVEN:
- treatment of COPD and asthma
side effects:
oral candidiasis
adrenal suppression
osteoporosis
Chlorpheniramine
Desloratidine
Fexofenadine
Hydroxyzine
anti-histamines H1 receptor antagonists
vasodilators bronchial smooth muscle
given:
Anaphylaxis
Hay fever
Urticaria
Sedation
side effects:
Drowsiness
Tinnitus
levodopa
dopamine precursor
Pro-drug
Crosses the blood brain barrier and is converted to dopamine
Striatal dopaminergic neurotransmission increased
given
parkinsons
side effects
Dyskinesia
Compulsive disorders
Hallucinations
Nausea
GI upset
