BETA BLOCKERS

SELECTIVE AND NON SELECTIVE

By:
JEWELYN D. CONOL
III-BSP
 SELECTIVE

• Beta-1 selective blockers are a

subclass of beta blockers that are
commonly used to treat high blood
pressure. Drugs in this class include:
 SELECTIVE

• GENERIC NAME: ATENOLOL

• BRAND NAME: TENORMIN
• DOSAGE: TABLET
• DOSAGE STRENGTH: 25mg, 50mg & 100mg
• PHARMACOKINETIC PROPERTY
 Absorption:
Bioavailability: 46-60%
Onset: Antihypertensive response, 3 hr
Duration: 12-24 hr (normal renal function)
Peak plasma time: 2-4 hr
 Distribution:
Protein bound: 6-16%
Vd: 50-75 L/kg
 Metabolism:
Metabolized to limited extent in liver
Metabolites: No clinically active metabolites
 Elimination:
Half-life: Children, 4.6 hr; adults, 6-7 hr; neonates, <35 hr; end-stage
renal disease, 15-35 hr
Dialyzable: Yes (HD)
Excretion: Feces (50%), urine (40-50%)
 SELECTIVE

• GENERIC NAME: METROPOLOL

• BRAND NAME: LOPRESSOR, TROPOL XL,
• DOSAGE & STRENGTH:
 Injectable sol’n(tartrate): 1mg/mL
 Tablet(tartrate): 25mg(generic)
50mg(generic&lopressor)
100mg(generic&lopressor)
 Tablet ER(succinate): 25mg, 50mg, 100mg,
200mg
 Capsule ER(succinate): 25mg, 50mg, 100mg,
200mg
• PHARMACOKINETIC PROPERTY
 Absorption:
Bioavailability: 40-50% (immediate-release) ; 65-77% (extended-release)
relative to immediate release
Onset: 20 min (IV), when infused over 10 min; onset may be immediate,
depending on clinical setting; 1-2 hr (PO)
Duration: 3-6 hr (PO); duration is dose-related; 24 hr (ER); 5-8 hr (IV)
Peak plasma time: 1.5-2 hr (immediate-release); 3.3 hr (extended-release)
Therapeutic range: 35-212 ng/mL
 Distribution:
Protein bound: 10%
Vd: 3.2-5.6 L/kg
 Metabolism:
Metabolized in liver by CYP2D6
Metabolites: Not active
 Elimination:
Half-life: 3-4 hr (average); 7.5 hr (poor metabolizers); 2.8 hr (extensive
metabolizers)
Dialyzable: Yes (HD)
Excretion: Urine 95%
 SELECTIVE

• GENERIC NAME: NEBIVOLOL

• BRAND NAME: BYSTOLIC
• DOSAGE: TABLET
• DOSAGE STRENGTH: 2.5mg, 5mg, 10mg, 20mg
• PHARMACOKINETIC PROPERTY
Absorption:
Bioavailability: Extensive metabolizers, 12%; poor
metabolizers, 96%
Peak plasma time: 1.5-4 hr
Distribution:
Protein bound: 98%
Vd: 8-12 L/kg
Metabolism:
Metabolized by CYP2D6 via alicyclic and aromatic
hydroxylation, N-dealkylation, glucuronidation
Elimination:
Half-life: Extensive metabolizers, 10-12 hr; poor
metabolizers, 19-32 hr
Excretion: Urine (38-67%), feces (13-44%)
 SELECTIVE

• GENERIC NAME: BISOPROLOL

• BRAND NAME: MONOCOR, ZEBETA
• DOSAGE: TABLET
• DOSAGE STRENGTH: 5mg, 10mg
• PHARMACOKINETIC PROPERTY
Absorption:
Bioavailability: 80%
Onset of action: 1-2 hr
Peak Plasma Time: 2-4 hr
Distribution:
Protein bound: 30%
Vd: 8-12 L/kg
Metabolism:
Hepatic
Elimination:
Half-Life: 9-12 hr (normal renal function); 27-36hr (<40
mL/min); 8-22 hr (hepatic cirrhosis)
Excretion: Renal (50%); feces (<2%)
 NON SELECTIVE

• Beta-1 selective blockers are a

subclass of beta blockers that are
commonly used to treat high blood
pressure. Drugs in this class include:
 NON SELECTIVE

• GENERIC NAME: SOTALOL

• BRAND NAME: BETAPACE, SORINE, SOTYLIZE
• DOSAGE & STRENGTH:
 Tablet: 80mg, 120mg, 160mg, 240mg
 Oral sol’n: 5mg/mL
 Injectable sol’n: 15mg/mL
• PHARMACOKINETIC PROPERTY
Absorption:
Bioavailability: 90-100%
Onset: IV, 1-2 hr; 5-10 min for ongoing VT
Peak plasma time: 2.5-4 hr
Distribution:
Protein bound: NONE
Vd: 1.2-2.4 L/kg
Metabolism:
Hepatic
Elimination:
Half-life: Adults, 12 hr; children, 9.5 hr; prolonged in
renal impairment
Excretion: Urine (unchanged)
 NON SELECTIVE

• GENERIC NAME: NADOLOL

• BRAND NAME: CORGARD
• DOSAGE & STRENGTH:
 Tablet: 20mg, 40mg, 80mg
• PHARMACOKINETIC PROPERTY
Absorption:
Bioavailability: 20-40%
Onset: 3-4hrs
Duration: 17-24hrs
Peak plasma time: 2-4 hr
Distribution:
Protein bound: 28-30%
Vd: 1.9 L/kg (1.88-2.02 L/kg)
Metabolism: NONE
Elimination:
Half-life: 10-24hrs
Excretion: Urine
Dialyzable: Yes (HD)
 NON SELECTIVE

• GENERIC NAME: PROPRANOLOL

• BRAND NAME: INDERAL, INDERAL LA,
HEMANGEOL, INNOPRAN XL
• DOSAGE & STRENGTH:
 Tablet: 10mg, 20mg, 40mg, 60mg, 80mg
 Oral sol’n: 20mg/5mL, 40mg/5mL
 Injectable sol’n: 1mg/mL
 Capsule ER: 60mg, 80mg, 120mg, 160mg
• PHARMACOKINETIC PROPERTY
 Absorption:
Bioavailability: 30-70% (food increases bioavailability)
Onset: Hypertension, 2-3 wk; beta blockade, 2-10 min (IV) or 1-2 hr
(PO)
Duration: 6-12 hr (immediate release); 24-27 hr (extended release)
Peak plasma time: 1-4 hr (immediate release); 6-14 hr (extended
release)
 Distribution:
Protein bound: 68% (newborns); 90% (adults)
Vd: 4 L/kg in adults
 Metabolism:
Metabolized by hepatic P450 enzymes CYP2D6 and CYP1A2
Metabolites: 4-hydroxypropranolol (active)
 Elimination:
Half-life: Children, 3.9-6.4 hr; adults, 3.9-6.4 hr (immediate release) or
8-10 hr (extended release)
Excretion: Urine (96-99%)
 NON SELECTIVE

• GENERIC NAME: PENBUTOLOL

• BRAND NAME: LEVATOL
• DOSAGE & STRENGTH:
 Tablet: 20mg
• PHARMACOKINETIC PROPERTY
Absorption:
Duration: >20hrs
Peak plasma time: 2-3hr
Peak plasma effect: 1.3-3hr
Distribution:
Protein bound: 80-90%
Metabolism:
Metabolism: Liver (oxidation and conjugation)
Elimination:
Half-life: 5hr
Excretion: Urine
 NON SELECTIVE

• GENERIC NAME: TIMOLOL

• BRAND NAME: BLOCADREN, TIMOL
• DOSAGE & STRENGTH:
 Tablet: 5mg, 10mg, 20mg
• PHARMACOKINETIC PROPERTY
 Absorption:
Bioavailability: 50%
Onset: (Hypotensive) 15-45min
Duration: 4hr
Peak plasma time: 1-2hr
Peak plasma effect: 0.5-2.5hr
 Distribution:
Protein bound: 60%
Vd: 1.7 L/kg in adults
 Metabolism:
Metabolism: Liver, extensive first-pass
 Elimination:
Half-life: 2-2.7hr
Excretion: Urine (15-20%)
Dialyzable: NO
REFERENCES