Clopamon Actions

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Actions of Clopamon in details

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.
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Clopamon stimulates motility of the upper gastrointestinal tract without stimulating gastric, biliary, or pancreatic secretions. While its mode of action is unclear, it appears to sensitize tissues to the action of acetylcholine. The effect on motility is not dependent on intact vagal innervation, but can be abolished by anticholinergic drugs. Clopamon increases the tone and amplitude of gastric (especially antral) contractions, relaxes the pyloric sphincter and the duodenal bulb, and increases peristalsis of the duodenum and jejunum resulting in accelerated gastric emptying and intestinal transit. It increases the resting tone of the lower esophageal sphincter. It has little, if any, effect on the motility of the colon or gallbladder.

The antiemetic properties of Clopamon appear to be a result of its antagonism of central and peripheral dopamine receptors. Dopamine produces nausea and vomiting by stimulation of the medullary chemoreceptor trigger zone (CTZ), and Clopamon blocks stimulation of the CTZ by agents like l-dopa or apomorphine, which are known to increase dopamine levels or to possess dopamine-like effects. Clopamon also abolishes the slowing of gastric emptying caused by apomorphine. Like the phenothiazines and related drugs, which are also dopamine antagonists, Clopamon produces sedation and may produce extrapyramidal reactions. Clopamon inhibits the central and peripheral effects of apomorphine, induces release of prolactin, and causes a transient increase in circulating aldosterone levels, which may be associated with transient fluid retention.

How should I take Clopamon?

Take Clopamon exactly as prescribed by your doctor. Clopamon is usually taken for only 4 to 12 weeks. Follow the directions on your prescription label.

NEVER TAKE Clopamon IN LARGER AMOUNTS THAN RECOMMENDED, OR FOR LONGER THAN 12 WEEKS.

High doses or long-term use of Clopamon can cause a serious movement disorder that may not be reversible. Symptoms of this disorder include uncontrollable muscle movements of your lips, tongue, eyes, face, arms, or legs. The longer you take Clopamon, the more likely you are to develop a serious movement disorder. The risk of this side effect is higher in women, diabetics, and older adults.

Take Clopamon 30 minutes before eating. Clopamon is usually taken before meals and at bedtime. Your doctor may want you to take the medication as needed only with meals that usually cause heartburn. Follow your doctor's instructions.

To take Clopamon orally disintegrating tablet (Clopamon):

  • Keep the tablet in its bottle or blister pack until you are ready to take the medicine. Make sure your hands are dry before handling a tablet. If the tablet breaks or melts in your hand, throw it away and use a new tablet.

  • Place the tablet on your tongue. It will begin to melt right away. Do not swallow the tablet whole. Allow it to melt in your mouth without chewing.

  • Swallow several times as the tablet melt. You do not need to drink liquid to help the tablet melt.

Do not take two different forms of Clopamon (such as tablets and oral syrup) at the same time.

Store Clopamon at room temperature away from moisture and heat. Keep the bottle tightly closed when not in use. After you stop taking Clopamon, you may have unpleasant withdrawal symptoms such as headache, dizziness, or nervousness. Talk to your doctor about how to avoid withdrawal symptoms when stopping the medication.

Clopamon 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. Clopamon is usually taken for only 4 to 12 weeks. Follow the directions on your prescription label.

NEVER TAKE Clopamon IN LARGER AMOUNTS THAN RECOMMENDED, OR FOR LONGER THAN 12 WEEKS. High doses or long-term use of Clopamon can cause a serious movement disorder that may not be reversible. Symptoms of this disorder include uncontrollable muscle movements of your lips, tongue, eyes, face, arms, or legs. The longer you take Clopamon, the more likely you are to develop a serious movement disorder. The risk of this side effect is higher in women, diabetics, and older adults.

Take Clopamon 30 minutes before eating. Clopamon is usually taken before meals and at bedtime. Your doctor may want you to take the medication as needed only with meals that usually cause heartburn. Follow your doctor's instructions.

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

To take Clopamon orally disintegrating tablet (ODT):

  • Keep the tablet in its bottle or blister pack until you are ready to take the medicine. Make sure your hands are dry before handling a tablet. If the tablet breaks or melts in your hand, throw it away and use a new tablet.
  • Place the tablet on your tongue. It will begin to melt right away. Do not swallow the tablet whole. Allow it to melt in your mouth without chewing.
  • Swallow several times as the tablet melt. You do not need to drink liquid to help the tablet melt.

Do not take two different forms of Clopamon (such as tablets and oral syrup) at the same time.

Store at room temperature away from moisture and heat. Keep the bottle tightly closed when not in use.

After you stop taking Clopamon, you may have unpleasant withdrawal symptoms such as headache, dizziness, or nervousness. Talk to your doctor about how to avoid withdrawal symptoms when stopping the medication.

Clopamon 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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Mechanism of Action

Clopamon stimulates motility of the upper gastrointestinal tract without stimulating gastric, biliary, or pancreatic secretions. The exact mechanism of action of Clopamon in the treatment of gastroesophageal reflux and acute and recurrent diabetic gastroparesis has not been fully established. It seems to sensitize tissues to the action of acetylcholine. The effect of Clopamon on motility is not dependent on intact vagal innervation, but it can be abolished by anticholinergic drugs.

Clopamon increases the tone and amplitude of gastric (especially antral) contractions, relaxes the pyloric sphincter and the duodenal bulb, and increases peristalsis of the duodenum and jejunum resulting in accelerated gastric emptying and intestinal transit. It increases the resting tone of the lower esophageal sphincter. It has little, if any, effect on the motility of the colon or gallbladder.

Pharmacodynamics

Cardiac Electrophysiology

In a randomized, double-blind, positive-controlled thorough ECG study in 48 healthy subjects, a single administration of 80 mg Clopamon nasal spray (approximately 5 times the recommended Clopamon dose) had no effect on the QTc interval.

Pharmacokinetics

Absorption

The absolute bioavailability of Clopamon following nasal administration of 10 mg Clopamon is 47% in healthy subjects compared to intravenous injection of Clopamon 10 mg. The systemic absorption after nasal administration is lower than that after oral administration given the same dose. Following nasal administration of Clopamon 15 mg in healthy subjects, the systemic exposure (Cmax and AUC) to Clopamon and the time to reach Cmax (Tmax) were similar to orally administered 10 mg Clopamon tablet.

After single nasal administration of Clopamon at doses ranging from 10 mg to 80 mg in healthy subjects, there was a dose-proportional increase in the mean values for Cmax and AUC.

The pharmacokinetic parameters of Clopamon in healthy subjects following a single nasal administration of Clopamon 15 mg are summarized in Table 3.

Table 3. Summary of Clopamon Pharmacokinetic Parameters in Healthy Subjects after a Single Nasal Administration of Clopamon 15 mg
Parameter * Clopamon

15 mg

*
Arithmetic mean (SD) except tmax for which the median (range) is reported.
N = 93
N 94
Cmax (ng/mL) 41.0 (19.9)
tmax (h) 1.25

(0.50 – 3.50)

AUC0-t (ng∙h/mL) 349 (174.7)
AUC0-inf (ng∙h/mL) † 367 (184.8)
t1/2 (h) 8.1 (2.0)

Distribution

Clopamon is not extensively bound to plasma proteins (about 30%). The whole body volume of distribution is high (about 3.5 L/kg), which suggests extensive distribution of drug to the tissues.

Elimination

The mean elimination half-life in individuals with normal renal function is approximately 8 hours for administration with Clopamon 15 mg.

Metabolism: Clopamon undergoes enzymatic metabolism via oxidation as well as glucuronide and sulfate conjugation reactions in the liver. Monodeethylmetoclopramide, a major oxidative metabolite, is formed primarily by CYP2D6, an enzyme subject to genetic variability.

Excretion: Approximately 85% of the radioactivity of an orally administered dose appeared in the urine within 72 hours. After oral administration of 10 or 20 mg, a mean of 18% and 22% of the dose, respectively, was recovered as free Clopamon in urine within 36 hours.

Specific Populations

Patients with Renal Impairment: In a study of 24 patients with varying degrees of renal impairment (moderate, severe, and end-stage renal disease [ESRD] requiring dialysis), the systemic exposure (AUC) of Clopamon following oral administration in patients with moderate to severe renal impairment was about 2-fold the AUC in subjects with normal renal function. The AUC of Clopamon in patients with ESRD on dialysis was about 3.5-fold the AUC in subjects with normal renal function.

Patients with Hepatic Impairment: In a group of 8 patients with severe hepatic impairment (Child-Pugh C), the average Clopamon clearance was reduced by approximately 50% compared to patients with normal hepatic function after administration of oral Clopamon.

Sex and Body Weight: The AUC0-t and Cmax of Clopamon were 34% and 42% higher in females than in males, respectively, following administration of Clopamon nasal spray to healthy subjects. Based on population pharmacokinetic analysis, lean body weight (34.3 to 93.5 kg) has a significant impact on Clopamon pharmacokinetics, with lower systemic exposure expected with higher lean body weight. The clinical significance of these findings is unknown.

Drug Interactions

Effect of Clopamon on CYP2D6 Substrates

Although in vitro studies suggest that Clopamon can inhibit CYP2D6, Clopamon is unlikely to interact with CYP2D6 substrates in vivo at therapeutically relevant concentrations.

Effect of CYP2D6 Inhibitors on Clopamon

Clopamon 20 mg was orally administered as a single dose to 24 healthy males, without (Period 1) and with (Period 2) a concomitant dose of fluoxetine 60 mg (a strong CYP2D6 inhibitor). Between the two periods, fluoxetine was administered orally for 8 days. The subjects who received concomitant Clopamon and fluoxetine had a 40% and 90% increase in Clopamon Cmax and AUC0-inf, respectively, compared to subjects who received Clopamon alone. The mean half-life for Clopamon was increased from 5.5 (±1.1) hours to 8.5 (±2.2) hours with concomitant fluoxetine.



References

  1. NCIt. "Metoclopramide: 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).
  2. EPA DSStox. "Metoclopramide: 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 Clopamon 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 Clopamon. 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.

User reports

6 consumers reported administration

When best can I take Clopamon, on an empty stomach, before or after food?
ndrugs.com website users have also released a report stating that Clopamon should be taken Empty stomach. In any case, this may not be the right description on how you ought to take this Clopamon. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Clopamon can be taken.
Users%
Empty stomach4
66.7%
After food1
16.7%
Before food1
16.7%


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Information checked by Dr. Sachin Kumar, MD Pharmacology

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