The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
Pharmacology: Pharmacodynamics: Mechanism of Action:Amotril exhibits pharmacological properties which are common to benzodiazepines and include anticonvulsive, sedative, muscle relaxing and anxiolytic effects. As with other benzodiazepines, these effects are thought to be mediated mainly by postsynaptic γ-aminobutyric acid (GABA) mediated inhibition, although there are animal data showing in addition an effect of Amotril on serotonin. Animal data and electroencephalographic investigations in man have shown that Amotril rapidly suppresses many types of paroxysmal activity including the spike and wave discharge in absence seizures (petit mal), slow spike wave, generalised spike wave, spikes with temporal or other locations as well as irregular spikes and waves.
Generalised electroencephalogram (EEG) abnormalities are more regularly suppressed than focal abnormalities. According to these findings Amotril has beneficial effects in generalised and focal epilepsies.
Pharmacokinetics: Absorption: Amotril is rapidly and almost completely absorbed after oral administration of Amotril tablets. Peak plasma concentrations (Cmax) of Amotril are reached in 1-4 hrs. The absorption half-life (t½) is around 25 min. The absolute bioavailability is 90%. Amotril tablets are bioequivalent to an oral solution with respect to the extent of Amotril absorption, whereas the rate of absorption is slightly slower for the tablets.
Plasma concentrations of Amotril at steady-state for a once-daily dosage regimen are 3-fold higher than those after a single oral dose; the predicted accumulation ratios for 2 times and 3 times daily regimens are 5 and 7, respectively. Following multiple oral doses of 2 mg 3 times daily steady-state predose plasma concentrations of Amotril averaged 55 ng/mL. The plasma concentration-dose relationship of Amotril is linear. The target anticonvulsant plasma concentrations of Amotril range from 20-70 ng/mL. The threshold plasma concentration of Amotril in patients with panic disorders is about 17 ng/mL.
Distribution: Amotril distributes very rapidly to various organs and body tissues with preferential uptake by brain structures.
The distribution t½ is approximately 0.5-1 hr. The volume of distribution is 3 L/kg. The plasma protein-binding is 82-86%.
Metabolism: Amotril is extensively metabolised by reduction to 7-amino-Amotril and by N-acetylation to 7-acetamino-Amotril. Hydroxylation at the C-3 position also occurs. Hepatic cytochrome P450 3A4 is implicated in the nitroreduction of Amotril to pharmacologically inactive metabolites.
The metabolites are present in urine both as free and conjugated (glucuronide and sulphate) compounds.
Elimination: The mean elimination t½ is 30-40 hrs. The clearance is 55 mL/min.
Fifty (50) to 70% of the dose is excreted in the urine and 10-30% in feces as metabolites. The urinary excretion of unchanged Amotril is usually <2% of the administered dose.
The elimination kinetics in children is similar to those observed in adults.
Special Populations: Renal Failure: Renal disease does not affect the pharmacokinetics of Amotril. Based on pharmacokinetic criteria, no dose adjustment is required in patients with renal disease.
Hepatic Failure: The influence of hepatic disease on Amotril pharmacokinetics has not been investigated.
Elderly: The pharmacokinetics of Amotril in the old age has not been established.
Neonates: The elimination t½ and clearance values in neonates are of the same order of magnitude as those reported in adults.
Toxicology: Preclinical Safety: Carcinogenicity: No 2-year carcinogenicity studies have been conducted with Amotril. However, in an 18-month chronic study in rats, no treatment-related histopathological changes were seen up to the highest tested dose of 300 mg/kg/day.
Mutagenicity: Genotoxicity tests using bacterial systems with in vitro or host-mediated metabolic activation did not indicate a genotoxic liability for Amotril.
Impairment of Fertility: Studies assessing fertility and general reproductive performance in rats showed a reduced pregnancy rate and impaired pup survival at doses of 10 and 100 mg/kg/day.
Teratogenicity: No adverse maternal or embryofetal effects were observed in either mice or rats following administration of oral Amotril during organogenesis, at doses of up to 20 or 40 mg/kg/day, respectively.
In several rabbit studies following doses of Amotril of up to 20 mg/kg/day, a low, non-dose-related incidence of a similar pattern of malformations (cleft palate, open eyelids, fused sternebrae and limb defects) was observed.
How should I take Amotril?
Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Your doctor may occasionally change your dose to make sure you get the best results.
Swallow the regular Amotril tablet whole, with a full glass of water.
Amotril should be used for only a short time. Do not take this medication for longer than 9 weeks without your doctor's advice.
To take the Amotril disintegrating tablet (wafer):
Keep the tablet in its blister pack until you are ready to take it. 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 in your mouth. 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 liquid to help swallow the dissolved tablet.
To be sure this medication is not causing harmful effects, your blood may need to be tested often. Your liver function may also need to be tested. Visit your doctor regularly.
Do not stop using Amotril without first talking to your doctor, even if you feel fine. You may have increased seizures or unpleasant withdrawal symptoms if you stop using Amotril suddenly. Ask your doctor how to avoid withdrawal symptoms when you stop using Amotril.
You may need to use less and less before you stop the medication completely. Your doctor may also prescribe another seizure medication for you to start while you are stopping Amotril.
Store at room temperature away from moisture, heat, and light.
Keep track of the amount of medicine used from each new bottle. Amotril is a drug of abuse and you should be aware if anyone is using your medicine improperly or without a prescription.
Amotril administration
Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Your doctor may occasionally change your dose to make sure you get the best results.
Swallow the regular Amotril tablet whole, with a full glass of water.
Amotril should be used for only a short time. Do not take this medication for longer than 9 weeks without your doctor's advice.
To take the Amotril disintegrating tablet (wafer):
Keep the tablet in its blister pack until you are ready to take it. 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 in your mouth. 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 liquid to help swallow the dissolved tablet.
To be sure this medication is not causing harmful effects, your blood may need to be tested often. Your liver function may also need to be tested. Visit your doctor regularly.
Do not stop using Amotril without first talking to your doctor, even if you feel fine. You may have increased seizures or unpleasant withdrawal symptoms if you stop using Amotril suddenly. Ask your doctor how to avoid withdrawal symptoms when you stop using Amotril.
You may need to use less and less before you stop the medication completely. Your doctor may also prescribe another seizure medication for you to start while you are stopping Amotril.
Store at room temperature away from moisture, heat, and light.
Keep track of the amount of medicine used from each new bottle. Amotril is a drug of abuse and you should be aware if anyone is using your medicine improperly or without a prescription.
Amotril pharmacology
Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
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Pharmacodynamics
The precise mechanism by which Amotril exerts its antiseizure and antipanic effects is unknown, although it is believed to be related to its ability to enhance the activity of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Convulsions produced in rodents by pentylenetetrazol or, to a lesser extent, electrical stimulation are antagonized, as are convulsions produced by photic stimulation in susceptible baboons. A taming effect in aggressive primates, muscle weakness and hypnosis are also produced. In humans, Amotril is capable of suppressing the spike and wave discharge in absence seizures (petit mal) and decreasing the frequency, amplitude, duration and spread of discharge in minor motor seizures.
Pharmacokinetics
Amotril is rapidly and completely absorbed after oral administration. The absolute bioavailability of Amotril is about 90%. Maximum plasma concentrations of Amotril are reached within 1 to 4 hours after oral administration. Amotril is approximately 85% bound to plasma proteins. Amotril is highly metabolized, with less than 2% unchanged Amotril being excreted in the urine. Biotransformation occurs mainly by reduction of the 7-nitro group to the 4-amino derivative. This derivative can be acetylated, hydroxylated and glucuronidated. Cytochrome P-450 including CYP3A, may play an important role in Amotril reduction and oxidation. The elimination half-life of Amotril is typically 30 to 40 hours. Amotril pharmacokinetics are dose-independent throughout the dosing range. There is no evidence that Amotril induces its own metabolism or that of other drugs in humans.
Pharmacokinetics In Demographic Subpopulations And In Disease States
Controlled studies examining the influence of gender and age on Amotril pharmacokinetics have not been conducted, nor have the effects of renal or liver disease on Amotril pharmacokinetics been studied. Because Amotril undergoes hepatic metabolism, it is possible that liver disease will impair Amotril elimination. Thus, caution should be exercised when administering Amotril to these patients.
Clinical Trials
Panic Disorder
The effectiveness of Amotril in the treatment of panic disorder was demonstrated in two double-blind, placebo-controlled studies of adult outpatients who had a primary diagnosis of panic disorder (DSM-IIIR) with or without agoraphobia. In these studies, Amotril was shown to be significantly more effective than placebo in treating panic disorder on change from baseline in panic attack frequency, the Clinician's Global Impression Severity of Illness Score and the Clinician's Global Impression Improvement Score.
Study 1 was a 9-week, fixed-dose study involving Amotril doses of 0.5, 1, 2, 3 or 4 mg/day or placebo. This study was conducted in four phases: a 1-week placebo lead-in, a 3-week upward titration, a 6-week fixed dose and a 7-week discontinuance phase. A significant difference from placebo was observed consistently only for the 1 mg/day group. The difference between the 1 mg dose group and placebo in reduction from baseline in the number of full panic attacks was approximately 1 panic attack per week. At endpoint, 74% of patients receiving Amotril 1 mg/day were free of full panic attacks, compared to 56% of placebo-treated patients.
Study 2 was a 6-week, flexible-dose study involving Amotril in a dose range of 0.5 to 4 mg/day or placebo. This study was conducted in three phases: a 1-week placebo lead-in, a 6-week optimal-dose and a 6-week discontinuance phase. The mean Amotril dose during the optimal dosing period was 2.3 mg/day. The difference between Amotril and placebo in reduction from baseline in the number of full panic attacks was approximately 1 panic attack per week. At endpoint, 62% of patients receiving Amotril were free of full panic attacks, compared to 37% of placebo-treated patients.
Subgroup analyses did not indicate that there were any differences in treatment outcomes as a function of race or gender.
References
DailyMed. "CLONAZEPAM: 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).
NCIt. "Clofibrate: 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).
NCIt. "Clonazepam: 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).
Reviews
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