This document provides an overview of metoprolol, a beta1-selective adrenergic receptor blocker used to treat hypertension, angina, arrhythmias, and migraine headaches. It discusses metoprolol's mechanism of action, pharmacokinetics, indications and uses, adverse effects, drug interactions, formulations, and dosage information. The document also references current research on metoprolol and beta blockers in general.

1. Ilkin Bakirli
SMU 3rd Year
23.03.2017
13. Metoprolol

2. 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

3. 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.

4. ATC classification
Category:
› sympatholytic
› antihypertensive
› antiarrhythmic
› adrenergic
C07AB02-
Metoprolol

5. 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

6. 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
›
›

7. Indications and uses
› Hypertension: used alone or as concomitant therapy with
thiazide-type diuretics, 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
›

8. 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

9. 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

10. 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

11. 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

12. Information for patients

13. 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)

14. 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_Classific
› 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=Metoprolo
› http://reference.medscape.com/drug/lopressor-toprol-xl-
metoprolol-342360#0