Antimin Actions

• Actions of Antimin in details
• Antimin administration
• Antimin pharmacology
• Antimin reviews

Actions of Antimin in details

Pharmacology: Antimin like other antihistamines acts via competitive blocking of H₁-histaminic receptors. Antimin penetrates very poorly into CNS. Therefore, it is devoid of significant CNS depressant effects. Antimin is highly selective antagonist of H₁-histaminic receptors. Antimin has very weak affinity for α-adrenoreceptors or acetylcholine receptors. In animal models, Antimin has very high affinity for H₁-histaminic receptors, which is greater than that of the terfenadine or astemizole. The antihistaminic effect persists for 18-24 hrs. In human subjects, Antimin suppresses wheal response to intradermally injected histamine. This action starts within 1-2 hrs of oral administration and maximum inhibitory effect evident in 2-4 hrs. The magnitude and duration of effects are dependent upon Antimin dose. On long-term administration, the drug retains its effectiveness without developing tachyphylaxis. In animal models, Antimin has also shown anti-serotonin activity. It also suppresses mast cell mediator release.

In addition, Antimin also possess anti-allergic activity which has been demonstrated in humans by skin prick and nasal challenge tests.

In human volunteers, Antimin did not reduce psychomotor performance as measured by sleep latency, symbol copying, digit symbol substitution, dynamic visual activity test or driving performance. In addition, Antimin does not potentiate the effects of centrally acting drugs eg, diazepam, ethanol and barbiturates.

Pharmacokinetics: Absorption: In humans, Antimin is rapidly absorbed after oral administration. There is a linear relationship between Antimin dose and both C_max and AUC. The 10, 20 and 40 mg of Antimin produce peak plasma concentrations of 5, 11, 28 mcg/L, respectively. Time to reach maximum concentration occurs between 1-1.5 hrs. After repeated dosing steady-state plasma concentrations occur by 5th day.

Metabolism: Antimin is metabolized to descarboethoxyloratadine (DCL) which is pharmacologically active.

Distribution: Antimin has extensive distribution in the body. The distribution t_½ of Antimin and DCL is 1.02 and 3.8 hrs, respectively.

Antimin is 97-99% bound to plasma proteins whereas DCL is 73-76% bound to plasma proteins. Small amount of both Antimin and DCL is secreted in breast milk, but the amount is minimal.

Elimination: Antimin undergoes extensive biotransformation. The elimination t_½ of Antimin after single dose is 8-11 hrs and that of DCL is 17-24 hrs. After multiple dosing, elimination t_½ of Antimin is 4.4 hrs and that of DCL is 8.7 hrs.

Pharmacokinetics of Antimin and that of DCL is not affected in patients with renal disease and in plasma patients on hemodialysis. In elderly patients too, disposition kinetics of Antimin and DCL is not affected. In patients of alcoholic liver disease, the t_½ of Antimin and that of DCL are longer but still within the range observed in a population of normal subjects.

How should I take Antimin?

Use exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended.

Antimin is usually taken once per day. Follow your doctor's instructions.

Do not crush, chew, or break the regular Antimin tablet. Swallow the pill whole.

Measure liquid medicine with a special dose-measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.

To take Antimin orally disintegrating tablet (Antimin, Alavert):

• Keep the tablet in its blister pack until you are ready to take the medicine. Open the package and peel back the foil from the tablet blister. Do not push a tablet through the foil or you may damage the tablet.

• Using dry hands, remove the tablet and place it on your tongue. It will begin to dissolve right away.

• Do not swallow the tablet whole. Allow it to dissolve in your mouth without chewing.

• Swallow several times as the tablet dissolves. If desired, you may drink water to help swallow the dissolved tablet.

Call your doctor if your symptoms do not improve.

Store at room temperature away from moisture and heat.

Antimin administration

May be administered without regard to meals.

Dispersible tablet: Place in mouth and allow to dissolve. Swallow with or without water.

Antimin pharmacology

Antimin is a long acting second generation antihistamine that is similar in structure to Antimin and azatadine. The pharmacology of Antimin is similar to other antihistamines, but unlike other H1-blockers, loratidine is shown to exhibit competitive, specific, and selective antagonism of H1 receptors. The exact mechanism of this interaction is unknown, but disposition of the drug suggests that Antimin's prolonged antagonism of histamine may be due to the drug's slow dissociation from the receptor or the formation of the active metabolite, desloratadine. Antimin does not penetrate the CNS effectively and has a low affinity for CNS H1-receptors.

References

1. DailyMed. "LORATADINE; PSEUDOEPHEDRINE SULFATE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
2. NCIt. "Loratadine: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
3. EPA DSStox. "Cyproheptadine: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

Reviews

The results of a survey conducted on ndrugs.com for Antimin are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Antimin. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.

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Information checked by Dr. Sachin Kumar, MD Pharmacology