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Beta blockers
- block beta-adrenergic
receptors
- some have selectivity for beta-1 or beta-2 receptors
- b-blockers are used to reduce cardiac work and
myocardial oxygen consumption.
- They bind to b1 adrenoreceptors
within the sino-atrial node and the myocardium,
- act to reduce the increase in heart rate and force of contraction
- during exercise
- times of anxiety
- they also improve myocardial perfusion by prolonging diastole
Affects
-
slow heart rate
-
depress myocardium
Drugs
- intrinsic sympathomimetic activity (less cold extremities)
- oxprenolol
- pindolol
- acebutolol
- celiprolol
- water-soluble (less psychiatric disturbance, more problems in renal
impairment)
- atenolol
- celiprolol
- nadolol
- sotalol (may prolong QT - avoid Hypokalaemia)
- vasodilating
- labetalol
- celiprolol
- carvedilol
- nebivolol
- cardioselective (beta-1 antagonism > beta-2)
- atenolol
- betaxolol
- bisoprolol
- metoprolol
- acebutolol
- short acting
Contra-indications
Side Effects
- heart
- fatigue, loss of joie de vivre
- subtle changes in exercise tolerance
- hypotension
- bradycardia
- heart failure
- conduction disorders
- peripheral CVS
- peripheral vasoconstriction
- coldness of extremities
- respiratory
- bronchospasm
- Use with caution in asthma & heart failure
- neuro
- GI disturbance
- metabolic
- reduction in glucose tolerance
- impaired response to hypoglycaemia
- Other
- exacerbations of Psoriasis
- Dry eyes
- corneal anaesthesia
- allergy
Side effects
- Intolerance
- fatigue
- cold extremities
- sexual dysfunction
- loss of motivation
- Bronchospasm: regardless of whether the drug used is cardioselective or
not
- CNS effects
- more common with lipid soluble drugs and include
- malaise
- vivid dreams
- nightmares
- hallucinations
- Masking of hypoglycaemia
- Metabolic disturbances
- increase plasma triglyceride
- decrease high density lipoprotein
Use
Pharmacokinetics
- well absorbed orally
- lipid soluble drugs e.g. metoprolol
- absorbed more rapidly by the gut, than the lipid insoluble drugs
- experience higher presystemic metabolism in the gut wall and the liver
- once in the circulation these drugs tend to be protein bound
- Polar b blockers
- excreted by the kidney without metabolism
- have longer half-lives
- not protein bound
- accumulate in renal failure
- Half-life of most b blockers is short such that
multiple daily dosing may be required
- b1 selective blockers are preferred
because there are less side effects
Dose
- Atenolol 50-200 mg daily
- Metoprolol 100-400 mg daily
- Bisprolol 5-20 mg daily
Interactions
- Anti-arhymthmics
- Antidepressants
- Antihypertensives
- Ca++ channel blockers
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