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Chemistry

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Also known as: 13523-86-9, Visken, Betapindol, Prinodolol, Carvisken, Durapindol
Molecular Formula
C14H20N2O2
Molecular Weight
248.32  g/mol
InChI Key
JZQKKSLKJUAGIC-UHFFFAOYSA-N
FDA UNII
BJ4HF6IU1D

Pindolol
A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)
Pindolol is a beta-Adrenergic Blocker. The mechanism of action of pindolol is as an Adrenergic beta-Antagonist.
1 2D Structure

Pindolol

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
1-(1H-indol-4-yloxy)-3-(propan-2-ylamino)propan-2-ol
2.1.2 InChI
InChI=1S/C14H20N2O2/c1-10(2)16-8-11(17)9-18-14-5-3-4-13-12(14)6-7-15-13/h3-7,10-11,15-17H,8-9H2,1-2H3
2.1.3 InChI Key
JZQKKSLKJUAGIC-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CC(C)NCC(COC1=CC=CC2=C1C=CN2)O
2.2 Other Identifiers
2.2.1 UNII
BJ4HF6IU1D
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Lb 46

2. Lb-46

3. Lb46

4. Prindolol

5. Visken

2.3.2 Depositor-Supplied Synonyms

1. 13523-86-9

2. Visken

3. Betapindol

4. Prinodolol

5. Carvisken

6. Durapindol

7. Pinbetol

8. Calvisken

9. Decreten

10. Pectobloc

11. Pynastin

12. Lb-46

13. Blocklin L

14. Glauco-visken

15. Pindololum

16. Blocklin-l

17. Dl-pindolol

18. Blockin L

19. Lb 46

20. (rs)-pindolol

21. 1-(1h-indol-4-yloxy)-3-[(1-methylethyl)amino]-2-propanol

22. 4-(2-hydroxy-3-isopropylaminopropoxy)-indole

23. 1-(1h-indol-4-yloxy)-3-(propan-2-ylamino)propan-2-ol

24. 1-(indol-4-yloxy)-3-(isopropylamino)-2-propanol

25. Apo-pindol

26. L-pindolol

27. 1-(1h-indol-4-yloxy)-3-(isopropylamino)propan-2-ol

28. 1-((1-methylethyl)amino)-3-(4-indolyloxy)-2-propanol

29. 4-(3-(isopropylamino)-2-hydroxypropoxy)indole

30. 2-propanol, 1-(1h-indol-4-yloxy)-3-[(1-methylethyl)amino]-

31. Dl-lb-46

32. 1-(1h-indol-4-yloxy)-3-((1-methylethyl)amino)-2-propanol

33. Bj4hf6iu1d

34. Nsc-757276

35. 2-propanol, 1-(4-indolyloxy)-3-(isopropylamino)-

36. Chebi:8214

37. 1-(1h-indol-4-yloxy)-3-[(1-methylethyl)amino]propan-2-ol

38. 2-propanol, 1-(1h-indol-4-yloxy)-3-((1-methylethyl)amino)-

39. Glauco-viskin

40. 1-(1h-indol-4-yloxy)-3-(propan-2-ylamino)-propan-2-ol

41. Ncgc00015786-11

42. 2-propanol, 1-(1h-indol-4-yloxy)-3-(1-methylethyl)amino-

43. (+-)-pindolol

44. Dsstox_cid_3476

45. Pindololum [inn-latin]

46. (-)-pindolol; (s)-(-)-pindolol; S-pindolol

47. Dsstox_rid_77043

48. Dsstox_gsid_23476

49. Dl-4-[2-hydroxy-3-(isopropylamino)propoxy]indole

50. Blocklin

51. Carvisken (tn)

52. Smr000059120

53. Blocklin-l (tn)

54. Visken (tn)

55. Ccris 9215

56. Hsdb 6539

57. Sr-01000000027

58. Einecs 236-867-9

59. Einecs 244-623-8

60. Unii-bj4hf6iu1d

61. Brn 1536506

62. Dl-4-(2-hydroxy-3-(isopropylamino)propoxy)indole

63. Dl-lb 46

64. Prestwick_397

65. Cas-13523-86-9

66. Pindolol [usan:usp:inn:ban:jan]

67. Spectrum_001109

68. (1)-1-(1h-indol-4-yloxy)-3-(isopropylamino)propan-2-ol

69. Pindolol [hsdb]

70. Pindolol [usan]

71. Pindolol [inn]

72. Pindolol [jan]

73. Pindolol [mi]

74. Pindolol [vandf]

75. (.+/-.)-pindolol

76. Prestwick0_000090

77. Prestwick1_000090

78. Prestwick2_000090

79. Prestwick3_000090

80. Spectrum2_001285

81. Spectrum3_000547

82. Spectrum4_000479

83. Spectrum5_001266

84. Pindolol [mart.]

85. Chembl500

86. Gtpl91

87. Pindolol [usp-rs]

88. Pindolol [who-dd]

89. Pindolol,(-)

90. P 0778

91. P-6820

92. Schembl5219

93. Lopac0_000955

94. Oprea1_770884

95. (+/-)-pindolol

96. Bspbio_000020

97. Bspbio_002193

98. Kbiogr_000958

99. Kbioss_001589

100. 5-21-03-00017 (beilstein Handbook Reference)

101. Mls000069496

102. Mls002548891

103. Divk1c_000837

104. Spectrum1500488

105. Pindolol (jp17/usp/inn)

106. Spbio_001289

107. Spbio_001959

108. Pindolol [orange Book]

109. 2-propanol, 1-(indol-4-yloxy)-3-(isopropylamino)-

110. Bpbio1_000022

111. Pindolol [ep Monograph]

112. 1-((1h-indol-4-yl)oxy)-3-(isopropylamino)propan-2-ol

113. Dtxsid8023476

114. Pindolol [usp Monograph]

115. Hms502j19

116. Kbio1_000837

117. Kbio2_001589

118. Kbio2_004157

119. Kbio2_006725

120. Kbio3_001693

121. Ninds_000837

122. 1-(1h-indol-4-yloxy)-3-[(propan-2-yl)amino]propan-2-ol

123. 2-propanol, 1-(indol-4-yloxy)-3-(isopropylamino)-, (+-)-

124. Hms1568a22

125. Hms1920h16

126. Hms2089i21

127. Hms2091p20

128. Hms2095a22

129. Hms3259i07

130. Hms3262p12

131. Hms3267k17

132. Hms3369e14

133. Hms3414j03

134. Hms3678h21

135. Hms3712a22

136. Hms3742c07

137. Hms3885n04

138. Pharmakon1600-01500488

139. Viskazide Component Pindolol

140. Hy-b0982

141. Pindolol, >=98% (tlc), Powder

142. Tox21_110221

143. Tox21_500955

144. Bdbm50019443

145. Ccg-39223

146. Nsc757276

147. Pdsp1_000771

148. Pdsp1_000772

149. Pdsp2_000759

150. Pdsp2_000760

151. (+/-)-pindolol-d7(iso-propyl-d7)

152. Akos015969756

153. Pindolol Component Of Viskazide

154. Tox21_110221_1

155. Cs-4473

156. Db00960

157. Lp00955

158. Nc00467

159. Nsc 757276

160. Sb17015

161. Sdccgsbi-0050929.p005

162. Idi1_000837

163. Ncgc00015786-06

164. Ncgc00015786-07

165. Ncgc00015786-08

166. Ncgc00015786-09

167. Ncgc00015786-10

168. Ncgc00015786-13

169. Ncgc00015786-14

170. Ncgc00015786-16

171. Ncgc00015786-20

172. Ncgc00015786-22

173. Ncgc00024925-03

174. Ncgc00024925-04

175. Ncgc00024925-05

176. Ncgc00024925-06

177. Ncgc00024925-07

178. Ncgc00261640-01

179. Bs-42390

180. Sbi-0050929.p004

181. 4-(3-isopropylamino-2-hydroxypropoxy)indole

182. Ab00052072

183. Eu-0100955

184. Ft-0673907

185. Sw196641-3

186. (+/-)-lb-46

187. C07445

188. C90604

189. D00513

190. Ab00052072-11

191. Ab00052072_12

192. Ab00052072_13

193. 1-(4-indolyloxy)-3-(isopropylamino)-2-propanol

194. 523p869

195. L000006

196. Q418101

197. 4-(2-hydroxy-3-isopropylaminopropoxy)indole

198. Sr-01000000027-2

199. Sr-01000000027-4

200. Sr-01000000027-5

201. Sr-01000000027-7

202. 1-(1h-indol-4-yloxy)-3-isopropylamino-propan-2-ol

203. Brd-a97701745-001-05-3

204. Brd-a97701745-001-09-5

205. 1-(1h-indol-4-yloxy)-3-(isopropylamino)-2-propanol #

206. Pindolol, European Pharmacopoeia (ep) Reference Standard

207. (+/-)-4-(2-hydroxy-3-(isopropylamino)propoxy)indole

208. 1-(1h-indol-4-yloxy)-3-isopropylamino-propan-2-ol(pindolol)

209. Pindolol, United States Pharmacopeia (usp) Reference Standard

210. 1-(1h-indol-4-yloxy)-3-isopropylamino-propan-2-ol((-)-pindolol)

211. N-(2-hydroxy-3-(1h-indol-4-yloxy)propyl)-n-isopropylamine

2.4 Create Date
2005-03-25
3 Chemical and Physical Properties
Molecular Weight 248.32 g/mol
Molecular Formula C14H20N2O2
XLogP31.8
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count3
Rotatable Bond Count6
Exact Mass248.152477885 g/mol
Monoisotopic Mass248.152477885 g/mol
Topological Polar Surface Area57.3 Ų
Heavy Atom Count18
Formal Charge0
Complexity248
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count1
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Information
1 of 2  
Drug NamePindolol
PubMed HealthPindolol (By mouth)
Drug ClassesAntianginal, Antihypertensive, Cardiovascular Agent
Drug LabelPindolol, a synthetic beta-adrenergic receptor blocking agent with intrinsic sympathomimetic activity is 1-(Indol-4-yloxy)-3-(isopropylamino)-2-propanol.C14H20N2O2 M.W. 248.32 Pindolol, USP is a white to off-white, crystalline powder having a f...
Active IngredientPindolol
Dosage FormTablet
RouteOral
Strength5mg; 10mg
Market StatusPrescription
CompanyMylan Pharms; Mutual Pharm

2 of 2  
Drug NamePindolol
PubMed HealthPindolol (By mouth)
Drug ClassesAntianginal, Antihypertensive, Cardiovascular Agent
Drug LabelPindolol, a synthetic beta-adrenergic receptor blocking agent with intrinsic sympathomimetic activity is 1-(Indol-4-yloxy)-3-(isopropylamino)-2-propanol.C14H20N2O2 M.W. 248.32 Pindolol, USP is a white to off-white, crystalline powder having a f...
Active IngredientPindolol
Dosage FormTablet
RouteOral
Strength5mg; 10mg
Market StatusPrescription
CompanyMylan Pharms; Mutual Pharm

4.2 Therapeutic Uses

Adrenergic beta-Antagonists; Anti-Arrhythmia Agents; Antihypertensive Agents; Serotonin Antagonists; Sympatholytics; Sympathomimetics; Vasodilator Agents

National Library of Medicine's Medical Subject Headings online file (MeSH, 1999)


A nonselective beta-adrenergic blocking agent with intrinsic sympathomimetic activity that is indicated in the management of hypertension.

Hussar, D.A. (ed.). Modell's Drugs in Current Use and New Drugs. 38th ed. New York, NY: Springer Publishing Co., 1992., p. 131


In the management of hypertension or chronic stable angina pectoris, many clinicians prefer to use low dosages of a beta1-selective adrenergic blocking agent (eg; atenolol, metoprolol), rather than a nonselective agent like pindolol, in patients with chronic obstructive pulmonary disease or insulin-dependent diabetes mellitus. However, selectivity of these agents is relative and dose dependent.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 1775


Pindolol ... /is/ indicated in the treatment of classic angina pectoris, also referred to as "effort-associated angina". /NOT included in US product labeling/

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 23rd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2003. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 550


For more Therapeutic Uses (Complete) data for PINDOLOL (6 total), please visit the HSDB record page.


4.3 Drug Warning

Contraindicted in patients with bronchial asthma, overt cardiac failure, cardiogenic shock, second and third degree heart block, and severe bradycardia. Adverse reactions include dizziness, fatigue, insomnia, edema, nausea, and muscle and joint pain. Use is best avoided in patients with bronchospastic diseases and therapy in diabetic patients must be closely monitored. When therapy is to be discontinued, the dosage should be gradually reduced over a period of 1 to 2 weeks.

Hussar, D.A. (ed.). Modell's Drugs in Current Use and New Drugs. 38th ed. New York, NY: Springer Publishing Co., 1992., p. 131


Abrupt withdrawal of pindolol may exacerbate angina symptoms or precipitate myocardial infarction in patients with coronary artery disease, or precipitate thyroid crisis in patients with thyrotoxicosis. Therefore, patients receiving pindolol (especially those with ischemic heart disease) should be warned not to interrupt or discontinue therapy without consulting their physician. When discontinuance of long term pindolol therapy is planned, particularly in patients with ischemic heart disease, dosage of the drug should be gradually reduced over a period of 1-2 wk. When pindolol therapy is discontinued, patients should be carefully monitored. If exacerbation of angina occurs or acute coronary insufficiency develops after pindolol therapy is interrupted or discontinued, treatment with the drug should be reinstituted promptly, at least temporarily, and appropriate measures for the management of unstable angina pectoris should be initiated. Because coronary artery disease is common and may be unrecognized, the manufacturers caution that it may be prudent not to discontinue pindolol therapy abruptly, even in patients being treated only for hypertension.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 1777


Pindolol should be used with caution in patients undergoing major surgery involving general anesthesia. The necessity of withdrawing beta-adrenergic blocking therapy prior to major surgery is controversial, but the manufacturers state that, if possible, pindolol should be withdrawn well before surgery. Severe, protracted hypotension and difficulty in restarting or maintaining a heart beat have occurred during surgery in some patients who have received beta-adrenergic blocking agents. If patients continue to receive pindolol prior to surgery, the anesthesiologist should be advised that the patient is receiving the drug. The manufacturers recommend administration of beta-agonists (eg; dopamine, dobutamine, isoproterenol) to reverse pindolol's beta-adrenergic blockade if necessary during surgery.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 1777


Pindolol should be used with caution and in reduced dosage in patients with impaired hepatic function.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 1777


For more Drug Warnings (Complete) data for PINDOLOL (14 total), please visit the HSDB record page.


4.4 Drug Indication

Pindolol is indicated in the management of hypertension. In Canada, it is also indicated in the prophylaxis of angina.


5 Pharmacology and Biochemistry
5.1 Pharmacology

Pindolol is a nonselective beta blocker indicated in the management of hypertension and prophylaxis of angina. It has a short duration of action as it is given twice daily, and a wide therapeutic window as doses can range from 10-60 mg/day. Patients should be counselled regarding the risk of cardiac failure, exacerbating ischemic heart disease with sudden withdrawal, nonallergic bronchospasm, masking hypoglycemia in diabetics, and masking hyperthyroidism.


5.2 MeSH Pharmacological Classification

Antihypertensive Agents

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)


Vasodilator Agents

Drugs used to cause dilation of the blood vessels. (See all compounds classified as Vasodilator Agents.)


Serotonin Antagonists

Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS. (See all compounds classified as Serotonin Antagonists.)


Adrenergic beta-Antagonists

Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety. (See all compounds classified as Adrenergic beta-Antagonists.)


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
PINDOLOL
5.3.2 FDA UNII
BJ4HF6IU1D
5.3.3 Pharmacological Classes
beta-Adrenergic Blocker [EPC]; Adrenergic beta-Antagonists [MoA]
5.4 ATC Code

C - Cardiovascular system

C07 - Beta blocking agents

C07A - Beta blocking agents

C07AA - Beta blocking agents, non-selective

C07AA03 - Pindolol


5.5 Absorption, Distribution and Excretion

Absorption

The mean oral bioavailability of pindolol is 87-92%. A 5 mg oral dose reaches a Cmax of 33.1 5.2 ng/mL, with a Tmax of 1-2 hours.


Route of Elimination

80% of an oral dose is eliminated in the urine, with 25-40% of the dose as the unchanged parent compound. 6-9% of an intravenous dose is eliminated in the feces. Overall, 60-65% of a dose is eliminated as glucuronide and sulfate metabolites.


Volume of Distribution

The volume of distribution of pindolol is approximately 2-3 L/kg.


Clearance

In otherwise healthy patients, the systemic clearance of pindolol is 400-500 mL/min. In patients with cirrhosis, the clearance of pindolol varies from 50-300 mL/min.


Pindolol is rapidly absorbed from the GI tract. Reported bioavailability ranges from 50-95%; bioavailability in uremic patients may be at the lower end of this range. Food does not reduce bioavailability but may increase the rate of GI absorption. Pindolol reportedly does not undergo substantial metabolism on first pass through the liver; ... only about 20% of an oral dose is metabolized on first pass. Peak plasma concentrations of 45-167 ng/ml are reached within 1-2 hr after administration of a single 20-mg dose. The extent of absorption may be decreased in patients with impaired renal function. The effect of pindolol on heart rate usually is seen within 3 hr and acute hemodynamic effects persist for 24 hr after administration of the drug.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 1778


Approximately 40-60% of pindolol is bound to plasma proteins. In healthy adults, the drug has an apparent volume of distribution of 1.2-2 l/kg; volume of distribution may be decreased by 50% in uremic patients. Pindolol is distributed into milk.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 1778


Elimination of pindolol appears to be a first-order process over a dose range of 5-20 mg. The drug has a plasma half-life of 3-4 hr in healthy adults. Plasma half-life increases to 3-11.5 hr in patients with renal failure, to 7-15 hr in geriatric patients, and varies from 2.5-30 hr in patients with hepatic cirrhosis. Approximately 60-65% of pindolol is metabolized in the liver to hydroxylated metabolites which are then excreted in urine as glucuronides and ethereal sulfates. In healthy adults, about 35-50% of the drug is excreted in urine unchanged; in patients with creatinine clearances less than 20 ml/min, less than 15% is excreted in urine unchanged.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 1778


Pindolol is rapidly and reproducibly absorbed (greater than 95%), achieving peak concentrations within 1 hr of drug administration ... The blood concentrations are proportional in a linear manner to the administered dose in the range of 5-20 mg ... Pindolol is only 40% bound to plasma proteins and is evenly distributed between plasma and red cells. The volume of distribution in healthy subjects is about 2 L/kg.

PDR; Physicians' Desk Reference Generics. 2nd Ed. Montvale, NJ: Medical Economics Co. p. 2489 (1996)


The polar metabolites are excreted with a half-life of approximately 8 hr and thus multiple dosing therapy ... results in a less than 50% accumulation in plasma. About 6%-9% of an administered intravenous dose is excreted by the bile into the feces.

PDR; Physicians' Desk Reference Generics. 2nd Ed. Montvale, NJ: Medical Economics Co. p. 2488 (1996)


5.6 Metabolism/Metabolites

30-40% of a dose of pindolol is not metabolized. The remainder is hydroxylated and subsequently undergoes glucuronidation or sulfate conjugation.


Pindolol reportedly does not undergo substantial metabolism on first pass through the liver; ... only about 20% of an oral dose is metabolized on first pass.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 1778


Approximately 60-65% of pindolol is metabolized in the liver to hydroxylated metabolites which are then excreted in urine as glucuronides and ethereal sulfates.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 1778


5.7 Biological Half-Life

The half life of pindolol varies from 3-4 hours but can be as high as 30 hours in patients with cirrhosis of the liver.


The drug has a plasma half-life of 3-4 hr in healthy adults. Plasma half-life increases to 3-11.5 hr in patients with renal failure, to 7-15 hr in geriatric patients, and varies from 2.5-30 hr in patients with hepatic cirrhosis

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 1778


5.8 Mechanism of Action

The beta-1 adrenoceptor is a G-protein-coupled receptor. Agonism of the beta-1 adrenoceptor allows the Gs subunit to upregulate adenylyl cyclase, converting ATP to cyclic AMP (cAMP). Increased concentrations of cAMP activate cAMP-dependant kinase A, phosphorylating calcium channels, raising intracellular calcium, increasing calcium exchange through the sarcoplasmic reticulum, and increasing cardiac inotropy. cAMP-dependant kinase A also phosphorylates myosin light chains, increasing smooth muscle contractility. Increased smooth muscle contractility in the kidney releases renin. Pindolol is a non-selective beta blocker. Blocking beta-1 adrenergic receptors in the heart results in decreased heart rate and blood pressure. By blocking beta-1 receptors in the juxtaglomerular apparatus, pindolol inhibits the release of renin, which inhibits angiotensin II and aldosterone release. Reduced angiotensin II inhibits vasoconstriction and reduced aldosterone inhibits water retention. Beta-2 adrenoceptors located in the kidneys and peripheral blood vessels use a similar mechanism to activate cAMP-dependant kinase A to increase smooth muscle contractility. Blocking of the beta-2 adrenoceptor relaxes smooth muscle, leading to vasodilation.


Class II antiarrhythmic, beta-adrenoceptor-blocking agents are membrane- depressant drugs that decrease the influx of sodium and calcium ions by reducing membrane-bound adenylate cyclase and cAMP. The reduction in cation transport lengthens depolarization by decreasing the amplitude and slope of the transmembrane potential. Beta-adrenoceptor-blocking agents also reduce myocardial contractility by decreasing calcium release from the sarcoplasmic reticulum (the influx of calcium couples excitation and contraction by initiating the release of calcium from the sarcoplasmic reticulum). Membrane-stabilizing activity enhances the reduction in myocardial contractility in overdose with these drugs in addition to producing a quinidinelike effect of QRS widening. A direct myocardial effect also leads to myocardial depression independent of beta-adrenergic blockade and membrane stabilization. /Class II beta-Blockers/

Ellenhorn, M.J. and D.G. Barceloux. Medical Toxicology - Diagnosis and Treatment of Human Poisoning. New York, NY: Elsevier Science Publishing Co., Inc. 1988., p. 191


The principal physiologic action of pindolol is to competitively block beta-adrenergic receptors within the myocardium (beta1-receptors) and within bronchial and vascular smooth muscle (beta2-receptors). In addition to inhibiting access of physiologic or synthetic catecholamines to the beta-adrenergic receptors, pindolol causes slight activation of the beta-receptors, making the drug a partial beta-agonist. This intrinsic sympathomimetic activity of pindolol differs from the beta-agonist activity of epinephrine and isoproterenol in that the maximum beta-adrenergic stimulation that can be obtained with pindolol is less. Other beta-adrenergic blocking agents can block pindolol's intrinsic sympathomimetic activity. Pindolol also has been shown to possess membrane-stabilizing activity or a quinidine-like effect, but this occurs only at plasma concentrations well above those obtained therapeutically. Unlike atenolol and metoprolol, pindolol is not a beta1-selective adrenergic blocking agent; pindolol is a nonselective beta-adrenergic blocking agent, inhibiting both beta1- and beta2-adrenergic receptors.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 1777


By inhibiting myocardial beta1-adrenergic receptors, pindolol produces negative chronotropic and inotropic activity. Both of these actions are reversed somewhat, but not entirely, by the drug's partial agonist activity. The negative chronotropic action of pindolol on the sinoatrial node results in a decrease in sinoatrial node discharge and recovery time, thereby decreasing stress- and exercise-stimulated heart rate. Pindolol has a lesser effect on resting heart rate than do beta-adrenergic blocking agents that do not possess intrinsic sympathomimetic activity, usually decreasing resting heart rate only by about 4-8 beats/min or not at all ... Pindolol has a lesser effect on resting cardiac output than on that stimulated by exercise. The decrease in myocardial contractility, blood pressure, and heart rate produced by pindolol during stress and exercise leads to a reduction in myocardial oxygen consumption which accounts for the effectiveness of the drug in chronic stable angina pectoris. Pindolol is probably not effective in patients who develop angina at rest or at low exercise levels.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 1778


Unlike other beta-adrenergic blocking agents, pindolol does not consistently suppress plasma renin activity. In some studies, the drug has increased plasma renin concentrations and reversed the suppression of plasma renin induced by other beta-adrenergic blocking agents. Pindolol has not been shown to cause sodium retention.

McEvoy, G.K. (ed.). American Hospital Formulary Service - Drug Information 2003. Bethesda, MD: American Society of Health-System Pharmacists, Inc. 2003 (Plus Supplements)., p. 1778


For more Mechanism of Action (Complete) data for PINDOLOL (7 total), please visit the HSDB record page.


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