MIXED α/β ADRENERGIC ANTAGONIST LABETALOLSpeaker:

BUSHRA KHAN

MIXED α/β ADRENERGIC ANTAGONIST

Alpha-Beta Adrenergic mixed blockers combine the effects of alpha and beta blocker medicines.

Common names of Alpha Beta blockers medicine are:

CARVEDILOL LABETALOL

LABETALOL

BRAND NAME: Normodyne, Trandate, Hybloc.

PHARMACOLOGICAL CLASS: α/β adrenergic blocker

THERAPEUTIC CLASS: Cardiovascular agent

ROUTES: Oral (p.o), IV

DOSAGE FORM: Tablets, Parentral.

PHARMACOLOGY / MECHANISM:

α blocker

β blocker

Decrease

HR/BP

INDICATIONS:

HYPERTENSION

PHEOCHROMOCYTOMA

DOSES:

Hypertension

Oral:I.D: 100mg po bid M.D: 200-400mg po bid.Parentral:Repeated IV Inj.: I.D: 20mg slow IV inj. with 2 min period.

ER Hypertension

Pheochromocytoma

Pediatric dose:PO:1-2mg/kg 12 hourly; may increase to 10mg/kg 6 hourlyIV:0.25-0.5mg/kg over 2 minutes repeated every 10 minutes if requiredFor infusion, 50mg/kg in 50ml of compatible IV fluid at

0-3ml/hr (0-3mg/kg/hr)

BIOAVAILABILITY 25%

PROTEIN BINDING 50%

METABOLISM Liver

HALF-LIFE 6-8hr tab 5.5hr IV

EXCRETION Urine

PHARMACOKINETIC DATA

CONTRAINDICATIONS:

Sinus bradycardia

Cardiogenic shock

Cardiac failure

Asthma

ADVERSE REACTIONS:Body as a Whole:  Tiredness, FatigueCardiovascular System:  Bradycardia, Cold extremities, Hypotension, Respiratory System:  Wheeziness,Digestive System: Diarrhea, Nausea, Hepatitis Nervous System:Dizziness, Vertigo, Light-headedness

DRUG INTERACTIONS:

MIXED α/β ADRENERGIC ANTAGONIST CARVEDILOLSpeaker:

MADIHA AHMED

CARVEDILOL

BRAND NAME: Coreg , Carvil, Dilatrend, Eucardic, Carloc.

PHARMACOLOGICAL CLASS: α/β Adrenergic blocker

THERAPEUTIC CLASS: Cardiovascular agent

ROUTES: Oral (p.o)

DOSAGE FORM: Tablets, Capsules .

PHARMACOLOGY / MECHANISM:

α blocker

β blocker

Decrease

HR/BP

INDICATIONS:

HYPERTENSION HEART FAILURE MYOCARDIAL INFARC

ANGINA LV DYSFUNCTIONCORONARY ARTERY

D

IRT:I.D: 6.25 mg po bid cf.M.D: 6.25 - 25 mg po bid cf.

ERC:I.D: 20 mg p.o od Max dose: 80 mg /day

IRT:I.D: 3.125 mg po bid for 2 weeks.

ERC:I.D: 10 mg po od for 2 weeks.

IRT:I.D: 6.25 mg po bid cf.M.D: 6.25 -25 mg po bid cf.Max dose: 50 mg/day

HypertensionHeart Failure Angina

DOSE:

IRT:I.D: 6.25 mg po bid .M.D: If tolerated, then increased to 12.5 mg bid

ERC:I.D: 20 mg po od .

L.V dysfunction

Pediatric Dose:0.08mg/kg 12 hrly; if tolerated, increase gradually to a maximum of 0.5-0.75mg/kg 12 hourly.

BIOAVAILABILITY 25-35%

PROTEIN BINDING 98%

METABOLISM Liver

HALF-LIFE 7-10 hours

EXCRETION Urine: 16%,Feces: 60%

PHARMACOKINETIC DATA

CONTRAINDICATIONS:

Severe bradycardia

Bronchial asthma

Cardiogenic shock

Hepatic impairment

Hypersensitivity

ADVERSE REACTIONSBody as a whole: FatigueCardiovascular System: Bradycardia, Hypotension, AnginaGastrointestinal System: Diarrhoea, Nausea, VomitingMusculoskeletal System: Arthralgia

DRUG INTERACTIONS: