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+

Acts in the DCT.
It is a competitive antagonist of aldosterone at the receptors in the DCT.
Decreased Na reabsorption and increased K reabsorption
= Increased Na loss and Diuresis.

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

α: Peripheral vasodilation

Sedation and muscle weakness (due to electrolyte abnm)
Antihypertensive,
Diuresis (in 3-4 days)
Potassium retention
Anti-androgenic effect- inhbn of ovarian androgen secretion
↑renal Ca excr, ↑plasma urea
Reversible hyperchloraemic MA

bioavailabilty rapid and extenisve absorption but high fi-rst pass metabolism leading to bioavailability of 25-35%

PO - BA 70%, extensive 1st pass metb. Onset 3-4hrs, dur upto 3 days

lipid solubility moderate

98% to albumin

90%

105 L/kg

Extensively hepatic, via CYP2C9, 2D6, 3A4, three
active metabolites

Hepatic: Rapidly and extensively metabolised by deacetylation and dethiolation. Active metab: canrenone and 7-alpha-spirolactone

faeces

Urine and faeces

7-8 hours

1-2hours, metab upto 24hrs

- Withdrawal.

- Care with: Opioids, Halo, OAD, CCB

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

↑K+(esp in renal failure). N/V and GI disturbances
Menstr irreg, Gynaecomastia
↑digoxin conc.
↓pressor response
↑effects of CVS depressants

Mixed alpha and beta blocker

Diuretic – Aldosterone antagonist

- used to reduce the excessive adrenergic activity that occurs in
response to heart failure.
- hypertension

Oedema – CHF, cirrhosis with ascites, refractory. HTN, Nephrotic syndrome. With loop/thiazide to conserve K+, diagn of Conn's syndr

third generation non selective beta blocker with alpha 1 antagonist
properties.

A synthetic steroid

Level 3

Level 3

oral form in both immediate and sustained release formulations

25/100mg tablets

oral
doses start at 6.25 BD and doubled 1/52 until not tolerated

PO. 25-200mg/day