Arotinolol
Arotinolol Uses, Dosage, Side Effects, Food Interaction and all others data.
Arotinolol is an alpha- and beta-receptor blocker developed in Japan. It is a thiopropanolamine with a tertiary butyl moiety. It has been studied for its potential to be an antihypertensive therapy. Artinolol is being developed by Sumitomo Pharmaceutical Co., Ltd. and it is currently under clinical trials.
Preclinical studies showed a lack of intrinsic sympathomimetic activities or membrane-establishing properties. It is confirmed that arotinolol presents vasorelaxant activity. This characteristic is also proved to be mainly mediated by its α1-blocking property. In preclinical hypertension trials, there is a specific acute bradycardiac and antihypertensive activity with a pronounced reduction in heart rate. Some reports indicate a delayed development of hypertension when arotinolol is administered daily. Arotinolol has a dose-dependent decrease in cardiac contractility and coronary blood flow as well as an increase in total peripheral resistance. The effects of arotinolol have been confirmed in clinical trials where this drug was able to decrease cardiac index and thus, blood pressure.
| Trade Name | Arotinolol |
| Generic | Arotinolol |
| Arotinolol Other Names | Arotinolol |
| Type | |
| Formula | C15H21N3O2S3 |
| Weight | Average: 371.53 Monoisotopic: 371.07959045 |
| Protein binding | The stereospecificity of arotinolol is very important for its pharmacokinetic characteristics. Arotinolol is highly bound to serum proteins reaching a ratio of the original dose of 95.3% in the form of the R-enantiomer and 84.5% of the S-enantiomer. The presented stereospecificity is thought to be related to the α1-acid glycoprotein. |
| Groups | Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Artinolol was introduced to be used as an antihypertensive agent since 1986. It has been studied for other functions like tremor control for patients with Parkinson disease and it is currently in clinical trials for its use in the control of blood pressure and heart rate.
How Arotinolol works
Arotinolol binds to the β1-, β2- and α1- adrenergic receptor sites with a very high affinity. Radioligand studies have shown that arotinolol presents a higher affinity to the β-receptor compared to the α-receptor. The elucidated mechanism of action seems to be the result of a reduction in the cardiac output via the β-blockade and an additional inhibition of the counter-regulatory increase in peripheral resistance mediated by the α-blockade.
Toxicity
The major toxic effects reported for arotinolol-like drugs are the presence of central nervous system depression.
Volume of Distribution
The stereospecificity of arotinolol is very important for its pharmacokinetic characteristics. The S-enantiomer is highly retained in red blood cells. The distribution studies have shown that arotinolol is mainly distributed from the plasma to the liver followed by the lungs and lastly in the heart. The distribution in the liver was independent on the stereochemistry of the molecules.
Elimination Route
Arotinolol gets rapidly absorbed and distributed in the plasma. The plasma concentration peaks 2 hours after initial administration.
Half Life
The reported half-life of arotinolol is 7.2 hours.
Elimination Route
The stereospecificity of arotinolol is very important for its pharmacokinetic characteristics. Both of the enantiomers were found in urine, suggesting this as the major elimination pathway. It is possible to find arotinolol in urine 2-4 hours after initial administration.
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