peristaltic motor activity of the gut is an essential ... · cyra ls tablet 10x10 systopic 9.90/tab...

Peristaltic motor activity of the gut is an essential activity for digestion and absorption and absorption of nutrients to sustained life

• Gut is made up of smooth muscles and smooth muscle contraction depends upon acetylcholine.

• Dopamine decreases the acetylcholine level while

• serotonin increases acetylcholinelevel,

• therefore dopaminergic and serotonergic activity balances the gut motility.

Receptors of GI Tract

SN Name of receptor Funtions

1 5 HT4 Receptors (seratonin) Lower Esophageal sphincter contraction, Ach Release, Peristalsis , Intestinal Mucosa secretion

2 D2 Receptors (dopamine)

Inhibition (delay gastric emptying time) LES relexation

5 HT receptors are found in cholinergic neuron in enteric nervous system where they induce release of acetyl choline which stimulate gastric emptying time motility.

Other factor affecting GI motility

Factors Affect On GI Motility

Food Intake

Clear fluid empty rapidly (+-30 min, Solid 1-2 hrs. Protein empties fast , followed by carbohydrate. Fat take long time.

PH of Stomach

Hyperacidity slows down GI Motility

Patient Factor

Pregnancy, Anxiety, Pain

Disease state diabetes mellitus

Gastroparesis, also called delayed gastric emptying, is a disorder that slows or stops the movement of food from the stomach to the small intestine. Normally, the muscles of the stomach, which are controlled by the vagus nerve, contract to break up food and move it through the gastrointestinal (GI) tract.

Diabetes is the most common known cause of gastroparesis. People with diabetes have high levels of blood glucose, also called blood sugar. Over time, high blood glucose levels can damage the vagus nerve.

46.5% of patients with IBS Also have GERD.

Requirement of compressive as well fast treatment for rapid relief

Introducing

Levosulpiride acts as a moderate agonist at the 5-HT4 receptor. This property, together with antagonism at D1 & D2 receptors, contribute to its gastrointestinal prokinetic effect.

Mode of Action

Rabeprazole belongs to a class of antisecretory compounds substituted benzimidazole. Rabeprazole suppress gastric acid secretion by inhibiting the gastric H+, K+ ATPase at the secretory surface of the gastric parietal cell. Rabeprazole blocks the final step of gastric acid secretion.

In gastric parietal cells.

Pharmacokinetic data of Rabeprazole

Parameters Rabeprazole Levosulpiride

Bioavailability 52% 30%

Metabolism Mostly non-

enzymatic partly

hepatic (CYP2C19

& CYP3A4)

Mostly by Hepatic

enzymatic reactions

Biological

Half-Life

1 – 1.5 hrs 9.7 hrs

Excretion 90%, Renal Renal

Parameters Levosulpiride

Domperidone Metoclopramide

Anti-emetic &

Prokinetic

Activity

More

Less

Less

Site of

prokinetic

action

Entire Gut Upper gut Upper Gut

Role in IBS-

Constipation Yes No No

Superior to Domperidone and Metoclopramide

Dosage :- As directed by Physician

Therapeutic Indications

•Functional Dyspepsia •Diabetic Gastroparesis •IBS with Constipation •GERD

Contraindications:-Epilepsy, Hyperprolactinaemia, GI Bleeding

Presentation:- 10X10 capsules MRP 82.00/10 Caps

Competitors for Rabopep L Capsules

Brand Name Packing Company MRP

Cyra LS Tablet 10x10 Systopic

9.90/Tab

Rabekind LS Cap 10x10 Mankind 8.80/Cap

Happi-L Cap 10x10 Zydus 13.00/Cap

Rekool -L Tab 10x10 Alembic 15.00/TAb

Rabifast-XL Cap 10x10 Zuventus 13.00/Cap

Rabicip-L Cap 10x10 Cipla 15.00/Cap