Tiapamil: Difference between revisions
CSV import |
CSV import |
||
| Line 1: | Line 1: | ||
'''Tiapamil''' is a [[calcium channel blocker]] used in the | {{Short description|A calcium channel blocker used in the treatment of cardiovascular diseases}} | ||
{{Drugbox | |||
| verifiedfields = changed | |||
| verifiedrevid = 477002123 | |||
| IUPAC_name = 2-(3,4-Dimethoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-2,3-dihydro-1H-isoindole-1,3-dione | |||
| image = Tiapamil.png | |||
| width = 200px | |||
| 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]]. | |||
==Pharmacology== | ==Pharmacology== | ||
Tiapamil | 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]]. | ||
==Clinical | ==Clinical Uses== | ||
Tiapamil is used in the | Tiapamil is used in the treatment of various cardiovascular conditions, including: | ||
* [[Hypertension]]: By reducing peripheral vascular resistance, tiapamil helps lower blood pressure. | |||
* [[Angina pectoris]]: It decreases myocardial oxygen demand by reducing heart rate and contractility. | |||
* [[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 | Common side effects of tiapamil include: | ||
* [[Dizziness]] | |||
* [[Headache]] | |||
* [[Nausea]] | |||
* [[Constipation]] | |||
Less common but more serious side effects may include: | |||
* [[Bradycardia]] | |||
* [[Hypotension]] | |||
* [[Heart failure]] | |||
== | ==Mechanism of Action== | ||
Tiapamil | 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== | ||
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. | |||
==Related pages== | |||
* [[Calcium channel blocker]] | * [[Calcium channel blocker]] | ||
* [[Verapamil]] | * [[Verapamil]] | ||
* [[Hypertension]] | * [[Hypertension]] | ||
* [[Angina pectoris]] | * [[Angina pectoris]] | ||
[[Category:Calcium channel blockers]] | [[Category:Calcium channel blockers]] | ||
[[Category: | [[Category:Cardiovascular drugs]] | ||
Revision as of 17:44, 18 February 2025
A calcium channel blocker used in the treatment of cardiovascular diseases
| Tiapamil | |
|---|---|
| File:Tiapamil.png | |
| INN | |
| Drug class | |
| Routes of administration | Oral |
| Pregnancy category | |
| Bioavailability | 40% |
| Metabolism | Hepatic |
| Elimination half-life | 3-4 hours |
| Excretion | Renal |
| Legal status | Rx-only |
| CAS Number | |
| PubChem | |
| DrugBank | |
| ChemSpider | |
| KEGG | |
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.
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.
Clinical Uses
Tiapamil is used in the treatment of various cardiovascular conditions, including:
- Hypertension: By reducing peripheral vascular resistance, tiapamil helps lower blood pressure.
- Angina pectoris: It decreases myocardial oxygen demand by reducing heart rate and contractility.
- Arrhythmias: Tiapamil can be used to manage certain types of cardiac arrhythmias due to its effects on cardiac conduction.
Side Effects
Common side effects of tiapamil include:
Less common but more serious side effects may include:
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
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.
