Tiapamil: Difference between revisions

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{{Short description|A calcium channel blocker used in the treatment of cardiovascular diseases}}
{{Short description|A calcium channel blocker}}
{{Drugbox
{{Drugbox
| verifiedfields = changed
| verifiedfields = changed
| verifiedrevid = 477002123
| verifiedrevid = 477002123
| IUPAC_name = 2-(3,4-Dimethoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-2,3-dihydro-1H-isoindole-1,3-dione
| IUPAC_name = 1-(3,4-Dimethoxyphenyl)-3-(3-(dimethylamino)propyl)-1,2,3,4-tetrahydroisoquinoline
| image = Tiapamil.png
| image = Dimeditiapramine.svg
| width = 200px
| image2 = Dimeditiapramine_3D_spacefill.png
| image2 = Tiapamil ball-and-stick model.png
| width2 = 200px
| tradename = Cardem
| legal_status = Rx-only
| routes_of_administration = Oral
| bioavailability = 40%
| protein_bound = 90%
| metabolism = Hepatic
| elimination_half-life = 3-4 hours
| excretion = Renal
}}
}}


'''Tiapamil''' is a [[calcium channel blocker]] that is primarily used in the management of [[cardiovascular diseases]]. It is a member of the [[phenylalkylamine]] class of calcium channel blockers, similar to [[verapamil]].
'''Tiapamil''' is a [[calcium channel blocker]] that is used in the treatment of [[cardiovascular disease]]. It is chemically related to [[verapamil]], another calcium channel blocker, but has distinct pharmacological properties.


==Pharmacology==
==Pharmacology==
Tiapamil functions by inhibiting the influx of calcium ions through [[L-type calcium channels]] in the [[cardiac muscle]] and [[vascular smooth muscle]]. This action results in the relaxation of vascular smooth muscle, leading to a decrease in [[vascular resistance]] and [[blood pressure]]. Additionally, it reduces the force of contraction of the heart, which can be beneficial in conditions such as [[angina pectoris]] and [[hypertension]].
Tiapamil functions by inhibiting the influx of calcium ions through [[voltage-gated calcium channels]] in the [[cardiac muscle]] and [[vascular smooth muscle]]. This action results in the relaxation of the smooth muscle and a decrease in [[myocardial contractility]], which can lead to a reduction in [[blood pressure]] and an improvement in [[angina]] symptoms.


==Clinical Uses==
==Mechanism of Action==
Tiapamil is used in the treatment of various cardiovascular conditions, including:
Tiapamil binds to the L-type calcium channels, which are responsible for the slow inward current of calcium ions during the [[plateau phase]] of the [[cardiac action potential]]. By blocking these channels, tiapamil reduces the force of contraction of the heart muscle and dilates the [[coronary arteries]], improving blood flow to the heart muscle.


* [[Hypertension]]: By reducing peripheral vascular resistance, tiapamil helps lower blood pressure.
==Clinical Use==
* [[Angina pectoris]]: It decreases myocardial oxygen demand by reducing heart rate and contractility.
Tiapamil is primarily used in the management of [[hypertension]] and [[angina pectoris]]. It may also be used in certain cases of [[arrhythmia]], where it helps to restore normal heart rhythm by slowing down the conduction of electrical impulses through the [[atrioventricular node]].
* [[Arrhythmias]]: Tiapamil can be used to manage certain types of cardiac arrhythmias due to its effects on cardiac conduction.


==Side Effects==
==Side Effects==
Common side effects of tiapamil include:
Common side effects of tiapamil include [[dizziness]], [[headache]], [[nausea]], and [[constipation]]. As with other calcium channel blockers, it may cause [[hypotension]] and [[bradycardia]]. Patients are advised to monitor their blood pressure regularly while on this medication.
 
* [[Dizziness]]
* [[Headache]]
* [[Nausea]]
* [[Constipation]]
 
Less common but more serious side effects may include:
 
* [[Bradycardia]]
* [[Hypotension]]
* [[Heart failure]]
 
==Mechanism of Action==
Tiapamil blocks the L-type calcium channels in the heart and blood vessels. This blockade prevents calcium from entering cells, which is necessary for muscle contraction. By inhibiting calcium entry, tiapamil causes relaxation of the vascular smooth muscle and decreases the contractility of the heart muscle.


==Pharmacokinetics==
==Chemical Properties==
Tiapamil is administered orally and has a bioavailability of approximately 40% due to first-pass metabolism in the liver. It is highly protein-bound (90%) and is metabolized hepatically. The elimination half-life of tiapamil is between 3 to 4 hours, and it is excreted primarily through the kidneys.
Tiapamil is a derivative of the [[isoquinoline]] class of compounds. Its chemical structure includes a 3,4-dimethoxyphenyl group and a dimethylamino propyl side chain, which contribute to its pharmacological activity.


==Related pages==
==Related pages==
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[[Category:Calcium channel blockers]]
[[Category:Calcium channel blockers]]
[[Category:Cardiovascular drugs]]
[[Category:Antianginal agents]]
[[Category:Antihypertensive agents]]

Latest revision as of 14:18, 21 February 2025

A calcium channel blocker


Tiapamil
INN
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Tiapamil is a calcium channel blocker that is used in the treatment of cardiovascular disease. It is chemically related to verapamil, another calcium channel blocker, but has distinct pharmacological properties.

Pharmacology[edit]

Tiapamil functions by inhibiting the influx of calcium ions through voltage-gated calcium channels in the cardiac muscle and vascular smooth muscle. This action results in the relaxation of the smooth muscle and a decrease in myocardial contractility, which can lead to a reduction in blood pressure and an improvement in angina symptoms.

Mechanism of Action[edit]

Tiapamil binds to the L-type calcium channels, which are responsible for the slow inward current of calcium ions during the plateau phase of the cardiac action potential. By blocking these channels, tiapamil reduces the force of contraction of the heart muscle and dilates the coronary arteries, improving blood flow to the heart muscle.

Clinical Use[edit]

Tiapamil is primarily used in the management of hypertension and angina pectoris. It may also be used in certain cases of arrhythmia, where it helps to restore normal heart rhythm by slowing down the conduction of electrical impulses through the atrioventricular node.

Side Effects[edit]

Common side effects of tiapamil include dizziness, headache, nausea, and constipation. As with other calcium channel blockers, it may cause hypotension and bradycardia. Patients are advised to monitor their blood pressure regularly while on this medication.

Chemical Properties[edit]

Tiapamil is a derivative of the isoquinoline class of compounds. Its chemical structure includes a 3,4-dimethoxyphenyl group and a dimethylamino propyl side chain, which contribute to its pharmacological activity.

Related pages[edit]