Beta1 selective blocker Metoprolol

13. Metoprolol

Ilkin Bakirli SMU 3rd Year 23.03.2017

13. Metoprolol

Presentation contents

Description and mechanism of action

ATC classification

Pharmacokinetics

Pharmacodynamics

Indications and use

Adverse effects and contraindications

Drug interactions

Formulations

Dosage and administration

Information for patient

Current research

Description and mechanism of action

Beta1 cardio-selective adrenergic receptor blocker

Beta1-receptor blockade results in a decrease in heart rate,
cardiac output and blood pressure.

ATC classification

Category:

sympatholytic

antihypertensive

antiarrhythmic

adrenergic

C07AB02-
Metoprolol

Pharmacokinetics

1. Adsorption: bioavailability= 50%, peak at 1-3hours after use

2. Distribution: 3.2L/kg-5.6L/kg

10% bound to albumen

Crosses placenta, found in breast milk and crosses BBB effectively

3. Metabolism: metabolised by CYP2D6

4. Elimination: by biotransformation in liver

Half life 3-4 hours

95% excreted in urine, 5% excreted in active metabolism

Pharmacodynamics

Unable to reverse beta2 vasodilation by epinephrine, unlike nonselective beta blockers

In asthmatic patients, reduces FEV1 and FVC lesser than nonselective beta blockers at equivalent dose

No intrinsic sympathomimetic activity

Slows sinus rate and decreases AV conduction

Indications and uses

Hypertension: used alone or as concomitant therapy with thiazide-typediuretics, at oral dosages of 100-450 mg daily.
Does not cause hypotension in healthy individuals.

Angina Pectoris: administered orally two or four times daily,
100-400 mg daily

Tachycardia/cardiac arrhythmias:

Heart failure: reduce mortality but may worsen congestive heart failure

Ischemic heart diseases: reduces CO, bradycardia

Anti-migraines: reduces headache

Adverse effects and Contraindications

Common/less serious: Fatigue, diarrhoea, dizziness, vivid dreams, ataxia, depression, vision problems, reduced blood flow on limbs, lowers alertness (cannot drive)

Serious: bradycardia, erectile dysfunction, hair loss, mood swing, dyslipidaemia, cardiac conduction abnormalities

Contraindications: asthma, COPD, liver diseases, alcohol, diabetes, psoriasis, myasthenia gravis, glaucoma, cardiogenic shock, hyperthyroidism, pheochromocytoma, haemodialysis, hyperlipidaemia, sinus bradycardia

Drug Interactions

Adrenaline and noradrenaline

Antihypertensive e.g: ACE inhibitors, calcium channel blockers, diuretics

Anti-arrhythmic

Anti-psychotics
increased risk of arrhythmias

Insulin

Aluminium salts, cholestyramine may decrease absorption

Formulations

Metoprolol tartrate: 100mg dose, Immediate release

Metoprolol succinate: 95mg dose, Slow release

Oral or IV

Salt based solution

Moderately lipophilic (CNS effect)

Soluble in water

Dosage and administration

25mg BD, 50mg BD, 100mg BD

Oral or IV

Twice daily

With or after meal

Eg; IV dose for MI:
early: 3 injections of 5mg with
2minute interval, tablet 50mg
every 6hours
late: 100mg twice daily

Information for patients

Current Research on beta blockers

Use in cancers (Melhem Bertrand et., Al 2011)

Reduce platelet aggregation (Bontel et., Al 2014)

Reduced risk of fractures (Toulis et., Al 2014)

Reduced post-acute traumatic brain injury (Alali et., Al 2014)

Thank you!

https://fr.slideshare.net/PrijayBakrania/the-pharmacology-of-betablockers

http://www.rxlist.com/lopressor-drug/clinical-pharmacology.htm

https://www.drugs.com/pro/metoprolol.html

https://en.wikipedia.org/wiki/Anatomical_Therapeutic_Chemical_Classification_System

Katzung, B.G., Masters, S.B., Trevor, A.J. Basic & Clinical Pharmacology, 13th Edition. The McGraw-Hill Companies, Inc., Lange, 2015, 158p-167p

http://druginfo.nlm.nih.gov/drugportal/dpdirect.jsp?name=Metoprolol

http://reference.medscape.com/drug/lopressor-toprol-xl-metoprolol-342360#0

3/10/2017

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Beta1 selective blocker Metoprolol