Dantrolene/parecoxib/methyldopa/ibutilide

Ketorolac High PO bioavailability 100+/-20% PPB 99% Vd 0.2L/kg. Hepatic (glucuronidation) Half life 5hr. Excreted unchanged in urine 5%.

Diclofenac PO bioavailability 50% PPB 99% Vd 0.17L/kg. (CYP2C9 mediated hydroxylation) Half life 4hr Excreted unchanged in urine <1%.

Neostigmine Onset 7min. Vd 0.7L/min 50% hepatic metabolism 1/10 antagonist activity of parent compound 50% elimination by kidney T (half) 1-2hr. Prolonged in renal function.

Edrophonium (dose 0.5mg/kg) Onset 1-2min. Vd 1.1L/min 30% hepatic metabolism. conjugation (inactive) 75% elimination dependent on kidney T(half) 2hr. prolonged in renal failure.

Pyridostigmine Onset 16min. Vd 1.6L/kg Minor Hepatic metabolism inactive metabolite. Renal excretion 80-90% unchanged from urine T(half)- 2hr prolonged in renal failure

Physostigmine Cross BBB Metabolism hepatic and hydrolysis by cholinesterase (ester linkage). Minimal renal excretion. T (half 15-40min)

Atropine Onset 1min. Duration 30-60min. Unpredictable oral absorption 50%PPB Liver metabolism inactive metabolite. 18% excreted unchanged in urine T (half)- 2.5hr

Glycopyrrolate Onset 2-3min. Duration 30-60min. Does not cross BBB/placenta 80% excreted unchanged in urine. T(half) 1.25hr. Elimination prolonged in uraemic patient

Hyoscine Cross BBB/placenta Extensive hepatic metabolism. (<1% excreted unchanged)

Propanolol No cardiac selectivity. No partial agonist activity 90-95% protein bound. Extensive first pass metabolism 75% Hepatic metabolism to active metabolites. Elim T(half) 2-3hr

Atenolol

Cardioselectivity. No partial agonist activity First pass metabolism 10%. Oral bioavailability ~60% 5% PPB . Vd 1L/kg >90% excreted unchanged in urine. Elim T(half 6-7hr)

Metoprolol Cardioselective. First pass metabolism 60%. Oral bioavailability 40%. PPB 10%. Vd 4L/kg Hepatic metabolism CYP2D6. Excreted unchanged in urine 10%. Elim T(half) 3hr

Esmolol Cardioselective. No partial agonism PPB 55%. Plasma hydrolysis. Elimination half T 0.15hr.

Sotalol (racemate. S form active) Oral bioavailability 60-100%. Minimal PPB. Vd 1L/kg. Excreted renal unchanged 70%. Elim half life 7hr.

Carvedilol (racemate. S-beta blockade. R and S both have equal alpha blockade activity) Oral bioavailability 25%. 95% PPB. Vd 1.5L/min. Elim T half -2-6hr. Extensive hepatic metabolism

Labetalol Alpha 1 blockade Non selective beta antagonism Partial beta 2 antagonism. Beta/alpha blocking potency ratio 3:1 oral/7:1 IV Conjugated to glucuronide. 5% recovered unchanged in urine. Elim T 5-8hr prolonged in hepatic failure.

Clonidine Oral bioavailability 95%. PPB 20%, Vd 2L/kg 50% metabolized in liver. The other half excreted unchanged Half life 12hr.

Sodium nitroprusside Onset in 30 sec. peak hypotensive effect in 2min. Offset of effect in 3min post stopping drug infusion. Metabolism release of cyanide and NO. Cyanide metabolized by liver rhodanese to form thiocyanate. Thiocyanate - renal excretion. Mean elimination T(half) is 3 days.

Glyceryl trinitrate Extensive first pass metabolism. Large Vd Elimination half life 1.5min

Hydralazine Low systemic bioavailability (16% fast acetylator, 35% slow acetylator) inactive metabolite N-Acetylated in liver. T (half) is 1hr. (but duration of hypotensive effect last 12hr. Dont know why)

Systemic clearance exceeds hepatic flow.Hydralazine rapidly combines with circulating alpha-ketoacid to form hydrazine. (Not very active)

Flecainide (class Ic) racemic mixture. Racemic mixture. Po bioavailability 70%, PPB 60%. Vd 5L/kg Half life 11hr. Metabolized by CYP2D6.

Amiodarone Po bioavailability ~30% PPB 99% Vd 66L/kg. Slow tissue accumulation need loading dose. half life 25 days. Metabolized by cyp3A4. (extensive) Active desethyl metabolite T (half) 61 days. Potent inhibitor of cyp3A4, 2C9, p-glycoprotein.

Ibutilide IKr blocker. Also activate inward Na current. cause Torsade Administered IV only. (extensive first pass metabolism). Hepatic metabolism T half average 6hr.

Lignocaine Well absorbed orally but variable first pass metabolism. Metabolite glycine xilidide (GX) and monoethyl GX less active Na channel blockade. Distribution half life 8min. Terminal elim T (half) 110min.

Digoxin Po bioavailability 70%. (intestinal flora may metabolize digoxin) 25% PPB. Vd 3-4L/kg.

T(half) 40hr. Urinary excretion ~80% unchanged, Metabolism occur by P-glycoprotein (amiodarone, flecainide decrease dig clearance)

Midazolam Po bioavailability 50%. 98% PPB Vd 1L/min. Hepatic metabolism cyp 3A4 active metabolite. Clearance 6ml/kg/min. T half 2hr.

Diazepam Po bioavailability 100%. 98%PPB. Vd 1L/kg. Hepatic metabolite 0 desmethyldiazepam and oxazepam. By CYP 2C19 and cyp 3A4. Clearance 0.4ml/min/kg, T half 43hr.

Warfarin (racemate) Oral bioavailability 100% 99% PPB Vd 0.15L/kg Hepatic metabolism 2C9 T (half) 40hr.

Acetylsalycylic acid Po bioavailability 70%. PPB 50%. Vd 0.15L/kg. T half 15-20min. Rapidly converted to salicylic acid. T half for this is 2-3hr. conjugated to glycine