You are on page 1of 16

Digoxin (Lanoxin/Lanoxicaps

)
Seth Adams
Duy Cao
Scott Davis
Cheryl Hanslovan
Bryan Ing
Kristin McKay
Vic Patel
Dan Rackham
Darren Smith
Phong Vuong

foxglove digitalis

General Structure .

. • Digoxin has an indirect effect on the sinoatrial and atrioventricular nodes (vagomimetic actions). • Baroreceptor sensitization also results from digoxin.Mechanism of Action • Digoxin inhibits membrane bound sodium-potassium ATPase resulting in an increased intracellular [Na +] and thus an increase in the intracellular [Ca 2+] by stimulation of Na+ and Ca2+ exchange. This leads to increased afferent inhibitory activity and reduced activity of the sympathetic nervous system and reninangiotensin system.

Digoxin Ca (-) 2+ 2K + + 3Na NaCaX ATPase 3Na + Ca2+ RyR ATP SR Contraction Ca 2+ ATPase Ca2+ ADP .

.Net Effect • Positive inotropic action (an increase in the force and velocity of myocardial systolic contraction). • Slowing of the heart rate and decreased conduction velocity through the AV node. • A decrease in the degree of activation of the sympathetic nervous system and reninangiotensin system.

Main Clinical Indications • Heart Failure – Increases cardiac output by positive inotropic actions – Therapeutic level of 0.5-2 mcg/L .5-1 mcg/L • Atrial Fibrillation – Rate control by vagomimetic actions – Therapeutic level of 0.

95) – 50 mcg ( red. 100 mcg ( yellow. # C2C) • Pediatric Elixer ( F = 0. # X3A ) • Capsules (Lanoxicaps) ( F = 0.7) – 125 mcg ( yellow.0 ) – 250 mcg per 1 ml (1 ml ampule) • Pediatric Injection ( F = 1.9 – 0. # B2C ).Available Dosage Forms • Tablets ( F = 0. and 200 mcg ( green. # Y3B ) or 250 mcg ( white.6 .75 – 0.85) – 50 mcg per 1 ml (10% alcohol) • Injection ( F = 1.0.0 ) – 100 mcg per 1 ml (1 ml ampule) . # A2C ) .

etc. halos around light • N&V and diarrhea (50-75% of patients) • Bradycardia (75-90% of patients) • Fatigue.Side Effects & Toxicities • Yellow/green visual changes. headache. malaise. • Anorexia . confusion.

Drug Interactions • Amiodarone – ↑[Digoxin] by 70% • Verapamil – ↑[Digoxin] by 50-75% • Propafenone – ↑[Digoxin] by 30% • Quinidine – ↑[Digoxin] by 50-75% • Erythromycin – ↑[Digoxin] .

Pharmacokinetic Parameters • Absorption – After oral dosing: • Onset of action in 0. but not into adipose tissue – Up to 25-30% is bound to plasma proteins • Metabolism – Follows first-order kinetics – Limited metabolism via sugar hydrolysis and lactone ring reduction – Half-life = 1-2 days • Excretion – 60-80% excreted unchanged in urine – Undergoes ACTIVE tubular secretion in the kidneys .5 – 2 hours • Peak effect reached in 2 – 6 hours • Distribution – Skeletal and heart muscle.

Clinical Considerations • Doses must be individualized and depends on the type & severity of the disease. renal function. and pulmonary disease • Patient must be advised not to take nonprescription cough or cold medications. and concomitant disease states • Normal dosage range is 125 – 500 mcg (50 – 200 mcg capsules) a day in a single dose • Contraindications: Patients w/ ventricular fibrillation. laxatives. hypercalcemia. or antidiarrheals without consulting the pharmacist or physician • Pregnancy category C . antacids. hypokalemia. age & weight of the patient. hypomagnesemia. renal impairment.

85 for females) • Clearance Digoxin: Cldig = (0.Digoxin Equations • IBW = 50 (or 45.06 to convert them from mL/min to L/hr) w/ co-administration of amiodarone: Cl = 0.3 L/kg x IBW – w/ renal dysfunction: Vd = (3.8 ml/min/kg x IBW) + CrCl – – • w/ CHF: Cl = (0.5 x Cl (without amiodarone) Vd = 7.3 x (inches over 60) • CrCl = ((140 .5) + 2.8 L/kg x IBW) + (3.33 ml/min/kg x IBW) + (0.Age) x IBW) / (72 x SCr) ( x 0.9 x CrCl) (these values were multiplied by 0.1 x CrCl) • LD = (Cp (desired level) x Vd) / (F) • MD = (Cp (desired level) x Cldig x Xo) / (F) .

4 mg/dL. He is 5’10” and weighs 73kg. B. and renal insufficiency.7 mcg/L for CHF . His SCr is 1.1 mg/dL. – Target Cpss = 0.Sample Problems • WB is a 75-year-old female with PMH including atrial fibrillation. Her SCr is 3. Calculate a dosing regimen using Lanoxicaps. – Target Cpss = 1. type II diabetes.0 mcg/L for atrial fibrillation • AS is a 78-year-old male with CHF. She is 5’4” and weighs 75 kg. hypertension. Calculate a loading and maintenance dose for Lanoxin tablets for Mrs.

7 kg (.5 kg + 2.7Xo = 80.3 (4 in) = 54.Problem Solutions .64 mcg  Use 375 mcg tabs once – MD = Cpss = 1 mcg/L = (X o(0.7) = 351.37 L/hr x 24 hr)  0.7 kg – CrCl = ((140-75) x 54.35 mL/min = 56.15 L – Cldig= (0.8 L/kg x 54.7 kg) + 3.7)) / (3.11 mL/min = 3.8 mL/min/kg x 54.35 mL/min – Vd = (3.15 L x 1 mcg) / (0.1 • WB w/ Renal Dysfunction: – IBW = 45.85)) / (3.7 kg) + 12.54 mcg  Use 125 mcg tabs qday .1 (12.88 mcg  Xo = 115.35 mL/min) = 246.4 x 72) = 12.37 L/hr – LD = (246.

95) = 392.95)) / (4.11 mcg  Use 100 mcg caps qday .33 mL/min/kg x 73 kg) + 0.Problem Solutions .3 (10 in) = 73 kg – CrCl = ((140-78) x 73 kg) / (1.15 mL/min – Vd = (7.3 L/kg x 73 kg) = 532.1 x 72) = 57.53 L/hr – LD = (532.0 kg + 2.7 mcg/L = (Xo(0.66 mcg  Use 400 mcg caps once – MD = Cpss = 0.1 mcg  Xo = 80.15 mL/min) = 75.52 mL/min = 4.53 L/hr x 24 hr)  0.2 • AS w/ Congestive Heart Failure: – IBW = 50.9 (57.7 mcg) / (0.9 L – Cldig= (0.95Xo = 76.9 L x 0.

2005. Updated Aug 12. 2006 from world wide web: http://www.com/cgi/rxlist. 2006 from world wide web: http://www.Lecs/Medicine. 2006. Connie Covington • Tharp. Retrieved March 9.rxlist. Updated March 12. (2006) Digoxin. Retrieved March 8.kr/Aldja/CVS/cardiac_glycoside/img/digoxin_structure.com/dig.html • Medicinal Plants.chunma. 11/3/2005.science.html • Rx-List. (2006) Digoxin Dosing.cgi?drug=digoxin • Digoxin Structure.rxkinetics. 2004. Retrieved March 8. Retrieved March 8. SFI Medical Publishing. R. (2006) Digoxin Image.References • 20th edition top 200 pharmacy drug cards.siu. 2006 from the world wide web: http://www. 2006 from world wide web: http://medpharm.edu/plantbiology/PLB117/Nickrent.GIF .ac. • Class lecture. Pharmacy 750.