CARDIOVASCULAR SYSTEM DRUGS-2
LVF = Left ventricular failure
U&Es = Urea and electrolytes
GFR = Glomerular filtration rate
t½ = Half-life
VTE = Venous thromboembolism
cGMP =Cyclic guanosine monophosphate
HMG CoA =3-hydroxy-3-methylglutaryl coenzyme A
MAO = Monoamine oxidas
DVT = Deep vein thrombosis
COMT = Catechol-O-methyl transferase
PE = Pulmonary embolism
VTE = Venous thromboembolism
OCP = Oral contraceptive pil
Fibrinolytics
EXAMPLES
Streptokinase, alteplase, reteplase, tenecteplase
MECHANISM OF ACTION
Activation of plasminogen to form plasmin, a proteolytic enzyme that promotes the breakdown of fibrin clots into fibrin degrading products leading to clot dissolution and reperfusion.
INDICATIONS
- Acute MI
- Massive pulmonary embolus (alteplase)
- Acute ischaemic stroke (under specialist supervision by stroke physician)
CAUTIONS AND CONTRA-INDICATIONS
- Aortic dissection.
- Active bleeding.
- Active peptic ulcer disease.
- Previous haemorrhagic stroke or recent ischaemic stroke.
- Coagulation defects.
- Recent surgery/trauma.
- Active intracranial neoplasm.
- Uncontrolled hypertension (relative contraindication)
SIDE-EFFECTS
- Bleeding (including cerebral haemorrhage).
- Nausea and vomiting.
- Reperfusion cardiac arrhythmias and ischaemia.
- Cerebral and pulmonary oedema.
- Anaphylaxis.
- Severe hypotension
METABOLISMANDHALF-LIFE
Variable–t½ for streptokinase is18–23min;t½ for alteplase is 4–5min. Metabolised predominantly by the liver.
MONITORING
Monitor for signs of bleeding, anaphylaxis and intracranial haemorrhage.
DRUG INTERACTIONS
- Risk of haemorrhage is increased with oral anticoagulants.
- Patients on ACEIs are at an increased risk of anaphylactoid reaction when streptokinase is administered
IMPORTANT POINTS
- Fibrinolytics are licensed for ST-elevation MI within 12h of the onset of chest pain (administered ideally within one hour).
- Streptokinase is derived from b-haemolytic Streptococci of Lancefield group C; persistence of antibodies to streptokinase may reduce the effect of subsequent doses. It has effectively been superseded by the newer fibrinolytics(e.g.reteplase)in acute mi(where primary percutaneous coronary intervention is not available).
- Alteplase is a recombinant tissue-type plasminogen activator.
- Does not cause allergic reactions and can be used in patients with recent streptococcal infections or recent use of streptokinase
Flecainide
MECHANISM OF ACTION
- Blocks Naþ dependent channels hence depressing phase 0 of the cardiac action potential.
- Increased PR and QRS intervals and lengthened ventricular refractory period lead to slower conduction of electrical impulses, with the greatest effect noted on the bundle of His and Purkinje system.
- In addition to the negative chronotropic effect, flecainide also reduces contractility.
INDICATIONS
- Wolff–Parkinson–White syndrome.
- AV nodal reciprocating tachycardia (AVNRT).
- Ventricular tachyarrhythmias
CAUTIONS AND CONTRA-INDICATIONS
- Second and third-degree AV block. SA node dysfunction. Impaired LV function.
- Long-standing AF. History of structural heart disease e.g. previous MI
SIDE-EFFECTS