Beta blockage leads to ↓Gs activity in receptor associated organs and
associated ↓in adenylyl cyclase and intracellular Ca2+.

Alpha blockage leads to ↓ Gq activation and subsequent ↓in IP3 and intracellular Ca2+

Beta blockage leads to ↓ Gs activity in receptor associated organs and
associated ↓ in adenylyl cyclase and intracellular Ca2+.

β: It produces
decreases in heart rate and cardiac output and myocardial oxygen consumption.

α: Peripheral vasodilation

It produces
decreases in heart rate and cardiac output and myocardial oxygen consumption

bioavailabilty complete absorption but high first pass metabolism results in bioavailability 25%

bioavailabilty Only available as IV therefore 100%

lipid solubility moderately lipid soluble, can enter CNS

lipid solubility is high so it crosses the BBB

50%

60% to albumin

3-16 L/kg

3.5 L/Kg

Hepatic, primarily via glucuronide conjugation

neither hepatic or renal!
by red blood cell esterases to a mostly inactive metabolite

Urine (60% as glucuronide conjugates, <5% as unchanged drug)

urine

6-8 hours

10 minutes

- Withdrawal.

- Care with: Opioids, Halo, OAD, CCB

- Due to its metabolism, it should be used in caution in liver failure patients and elderly

- Care with: Opioids, Halo, OAD, CCB

- It is an irritant to veins and may lead to tissue necrosis with extravasation

It is a racemic solution with four stereoisomers present in
equal proportions. The SR isomer is likely responsible for the alpha blocking
effects and the RR isomer for the betablockade

Mixed alpha and beta blocker

Ultra-short-acting selective beta1-adrenoceptor antagonist; Vaughan Williams class II antiarrhythmic.

- Used in the setting of an acute hypertensive crisis
- Pregnancy related hypertension

- Short term management tachycardia and hypertension in a monitored patient
- For SVT termination

- No intrinsic sympathomimetic activity or membrane stabilising properties

an alpha 1 blocker and a non selective beta blocker.

Cardio-selective beta blocker with rapid onset and off-set.

Level 2

Level 2

available as a 50-400mg tablets and as a colourless solution containing 5mg/ml.

only available as an IV formulation.
presented as a clear liquid usually at a concentration of 10mg/ml

IV and oral
doses IV in 20mg pushes, oral for HTN 100-400mg BD

IV
dose In 10mg increments titrate to eff¬ect