Benzimidazole derivative: Domperidone
Effect : stimulates peristalsis of the digestive tract, increases cardiac sphincter tone and increases the amplitude of pyloric sphincter expansion after meals, but does not affect gastric secretion.
– Indication
+ Treatment of severe nausea and vomiting (especially in people taking cytotoxic drugs).
+ Nausea and vomiting, feeling of bloating and indigestion after eating due to slow food moving down the intestines.
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Contraindications : postoperative vomiting, gastrointestinal bleeding, children under 1 year old and do not use regularly for a long time.
Preparation and dosage
+ Motilium : adults take 3-4 times/day, 10-20mg each time, 15 minutes before meals. Severe patients inject intravenously 1-2 tubes/day. Children take 1/2 teaspoon/10kg of oral suspension, before meals or insert 4mg/kg/day rectally, divided into several times.
Tablets: 10mg
Oral suspension: 30mg/30ml Suppository: 30mg
Injection 2ml: 10mg
+ Elitan (metoclopramide) : adults take 10mg/time, 3 times a day. Children 2-7 years old = 1/2 adult dose or suppository 0.5mg/kg/day, children < 2 years old take 0.5mg/kg/day divided into 3 times.
Oral solution 5ml: 5mg Tube 2ml: 10mg
Suppositories: 10mg, 20mg
5.2. Gastrointestinal parasympathomimetic drug “Cisapride”
Effect
+ Increased esophageal motility, increased pressure through the cardia.
+ Increases gastric-duodenal motility, quickly empties the stomach.
+ Increases movement of stomach - small intestine - large intestine.
Indications: esophageal reflux, indigestion
Preparation and dosage
+ Prepulsid (cisapride) : adults take 10mg/time 15-30 minutes before meals, 4 times a day. Children 0.15-0.3mg/kg/day, divided into 4 times. Tablets: 10mg, 20mg
+ Esorid (cisapride) : adults take 5mg/time, 2-3 times/day. Children take 1/2 tablet/time, 2 times/day. Tablets: 5mg.
5.3. Drugs acting on the enkephalinergic system
Enkephalinergic receptors in the intestine regulate intestinal motility by stimulating hypokinetic muscles and inhibiting spasms in hyperkinetic muscles.
Trimebutine (dibridate)
+ Mechanism: stimulates enkephalinergic receptors in the intestine when there is a disorder
+ Indications: postoperative ileus, gastrointestinal dysfunction (abdominal pain, spasm, indigestion, diarrhea or constipation).
+ Dosage: Adults take 3 times a day, 1 tablet or 1 tablespoon of suspension/time or insert 1 - 2 suppositories. Intramuscular or intravenous injection when there is acute pain. Children take 1/2 - 1 tablespoon of syrup/time, 2-3 times/day, depending on age.
Tablet or suppository: 100mg 5ml tube: 50mg
250ml bottle: 1.2g powder for oral suspension
Racecadotril (hydrasec )
Reduces intestinal secretion and electrolytes of intestinal mucosa when inflamed or stimulated by bacterial toxins (no effect on normal intestine).
Often used in acute diarrhea. Adults take 1 tablet initially, then 1 tablet every 8 hours, not more than 4 tablets/day. Not for use in children < 15 years old.
Capsule: 100mg
6. Antispasmodic and anti-motility drugs
Due to their antispasmodic effects on smooth muscle by different mechanisms, the drugs are used to treat pain caused by spasms of the digestive tract, biliary tract, and genitourinary tract.
6.1. Peripheral parasympatholytic drugs (drugs that do not enter the central nervous system due to the presence of quaternary amines)
Buscopan : adults take 1 - 2 pills/time, 3 - 5 times/day or inject (intramuscular, subcutaneous, intravenous) 1 tube/time, several times/day. Children inject 1/4 tube/time, 3 times/day.
Tablets: 10mg 1ml tube: 20mg
Luostyl (difemerin) : adults take 3 - 4 tablets/day. Intramuscular injection 1 - 3 tubes/day Capsules: 2.5mg, 1ml tube: 1mg
6.2. Direct antispasmodic drugs
Mebeverine
+ Synthetic drug, antispasmodic effect on smooth muscle in the digestive tract and biliary tract.
+ Indications: intestinal spasms (colon), biliary tract pain
+ Dosage: Adults take 1 tablet/time, 4 times a day (20 minutes before meals), then use a maintenance dose of 1-2 tablets/day. Can be used for people with glaucoma and prostate cancer. Coated tablets or capsules: 100mg
Phloroglucinol (spasfon): adults take 6 tablets/day divided into 2-3 times Tablets or suppositories: 40mg, 80mg, 150mg
Alverin ( spasmaverin)
Antispasmodic of smooth muscle of digestive tract, urinary tract and blood vessels, 3 times stronger than papaverine, toxicity = 1/3 papaverine. Adults take 40 - 60 mg/time, 3 - 4 times/day or insert 1 - 2 suppositories/day.
Tablets or capsules: 40mg, 60mg
Drotaverine (nospa ): adults take 40 - 80mg/time, 3 times a day. Subcutaneous injection 1 - 2 tubes/time, 1 - 3 times a day or intravenous injection 1 - 2 tubes.
Tablets: 40mg Tube 2ml = 40mg
Can be injected into the artery in case of peripheral vasospasm.
7. Antidiarrheal drugs
In addition to treating diarrhea with antibiotics, symptomatic drugs are also used, such as antisecretory drugs (because they cause electrolyte loss) and anti-intestinal motility drugs (because they cause diarrhea and pain).
7.1. Adsorbents, covering the intestinal mucosa
Drugs that can bind to proteins of the digestive mucosa form a thin layer covering the mucosa.
Medicines
+ Smecta : see section on drugs for treating stomach ulcers.
+ Actapulgite : in addition to protecting the intestinal mucosa, the drug also absorbs bacterial toxins and gases in the intestine. Adults take 3 packets/day (2 hours away from other drugs). Children take 1/2 packet/time, 2-3 times/day. Powder packet: 3g
7.2. Substances that reduce intestinal secretion and decrease intestinal motility
It is a synthetic drug that acts like morphine because it has a structure similar to morphine.
Effect
+ Reduces intestinal motility, prolongs intestinal transit time, reduces digestive secretions.
+ Increases the transport of water and electrolytes from the intestine into the blood.
+ Increased anal sphincter tone.
Assign
+ Treatment of acute non-infectious diarrhea after rehydration and electrolyte replacement with ORS.
+ Treatment of chronic diarrhea due to intestinal dysfunction, colitis.
Contraindications : children under 13 years old, infectious diarrhea, pseudomembranous colitis.
Preparation and dosage
+ Loperamide (altocel) : 2mg cylindrical capsules, take 2 tablets at first, then take 1 tablet every 4 hours, no more than 4 tablets per day.
+ Loperamide oxide (arestal) : is a precursor of loperamide, adults take 2mg initially, then 1mg after each bowel movement until diarrhea stops. Maximum 8mg/day. Do not use for children < 12 years old.
+ Diphenoxylate (diarsed ): tablets containing 2.5mg diphenoxylate + 0.025mg atropine sulfate, initially take 2 tablets, supplement with 1 tablet/time, no more than 6 tablets/day.
7.3. Bacteria and fungi
7.3.1. Lactobacillus acidophilus
Bacteria produce lactic acid and two bactericidal substances: lactocidin and acidophillin. Capable of synthesizing B vitamins.
Normally, in the intestine, there is a balance between sucrose-destroying bacteria and protein-destroying bacteria. When substances attack sucrose-destroying bacteria such as alcohol, stress, infection, antibiotics... it will cause an imbalance, increasing protein-destroying bacteria, leading to digestive disorders (diarrhea, constipation, bloating).
Lactobacillus acidophilus has the following effects:
+ Restore the balance of symbiotic bacteria in the intestine.
+ Stimulates the growth of sucrose-degrading bacteria.
+ Non-specific immune stimulation of intestinal mucosa
+ Antibacterial
Indication: treatment of diarrhea caused by intestinal dysbiosis
Preparation and dosage
+ Antibio : 1g powder packet contains 100,000,000 (10 8 ) live bacteria. Adults take 3 packets a day, divided into 3 times. Children take 2 packets a day, divided into 2 times. Bacteria can live for 2 days in gastric juice, 5 days in the intestines and 8 days in the duodenum.
+ Lacteol (contains bacteria killed by heat)
0.5g tablet contains 450,000,000 lactobacilus acidophilus bacteria, 7ml tube contains 350,000,000 bacteria
Adults take 2 tubes/time, 4 times/day or 5 pills/time, 3-5 times/day. Children with acute diarrhea take 1 tube/time, 4 times/day or 3 pills/time, 5 times/day.
7.3.2. Saccharomyces boulardii
Yeast has the following effects:
+ B vitamins (B 1 , B 2 , B 6 , PP)
+ Invivo and invitro bacteriostatic
+ Kills candida albicans
Indication
+ Preventive treatment of antibiotic-induced diarrhea.
+ Acute diarrhea in all ages.
Because yeast is a living cell, it should not be taken with water that is too hot (> 50 0 C), too cold or contains alcohol.
Preparation: Ultra – Levure capsules contain 56.5mg of freeze-dried bacteria, take 1 capsule/time, 4 times a day
VALUATION
1. Describe the effects, mechanisms, and indications of drugs for treating gastric and duodenal ulcers?
2. Describe the effects and contraindications of drugs that regulate gastrointestinal motility?
3. Describe the effects and indications of direct antispasmodic drugs?
4. Describe the effects and indications of bacterial and fungal products that have antidiarrheal effects?
MEDICATIONS FOR RESPIRATORY DISORDERS
Target:
1. Describe the effects, indications and dosage of expectorants.
2. Describe the effects, indications and dosages of cough medicines.
3. Describe the effects, indications and dosages of asthma medications.
1. Drugs that alter bronchial secretions
– Bronchial fluid is secreted from:
+ Goblet cells secrete viscous, oily fluid due to the presence of mucoprotein and mucopolysaccharide, and are not controlled by nerves.
+ Secretory glands of the mucosa and serosa, have liquid. Innervated by many autonomic nerves.
+ In addition, there is also a liquid permeate of the bronchial wall.
– Bronchial mucus is a natural lubricant of the respiratory tract mucosa. Mucus has the effect of adhering to dust particles and bacteria, then thanks to the cilia system, pushing them out.
– Normally, excess fluid is evaporated by air or absorbed. But most of it is transferred to the trachea by cilia and falls into the digestive tract. The volume of fluid is usually from 1 – 10ml/kg/24 hours depending on the species and season.
1.1. Drugs that reduce secretion
– Parasympatholytic drugs (atropine),
– H1 antihistamines .
Rarely used clinically because it makes secretions thick, difficult to expel and easily causes alveolar collapse.
1.2. Expectorant
1.2.1. Drugs that thin secretions : drugs that work by two mechanisms:
Stimulates receptors from the gastric mucosa to cause parasympathetic reflexes to increase secretion in the respiratory tract. At therapeutic doses, it often causes stomach irritation and can cause vomiting. Drugs include:
+ Sodium iodide and potassium iodide, take 1-2g/day. Long-term use causes iodine accumulation so it is almost never used today.
+ Oral sodium benzoate 1-4g/day, long-term use causes sodium accumulation
+ Ammonium acetate 0.5 - 1g/day, not for people with liver or kidney failure.
+ Ipeca or ipecacuanha: in case of cough and phlegm use low dose (maximum 1.4mg), high dose causes vomiting. Active ingredient is in Dessessartz syrup.
The above drugs are rarely used today.
Direct stimulation of secretory cells: often using volatile essential oils such as terpin (distilled from terebenthin essential oil), gaicol, eucallyptol. These essential oils also have
Antiseptic effect. Do not use garcinia cambogia essential oil for children < 30 months old.
1.2.2. Mucolytic drugs (expectorants)
1.2.2.1. N – acetylcysteine
BD: Mycomyst, acemux, exomux, mitux, meko, mucosol, mysoven…
– Effect
+ Changes the structure and reduces the viscosity of mucus, so mucus "plugs" can easily move out of the respiratory tract through the cough and expectoration reflex.
+ Acetylcysteine and drugs with free thiol groups have the effect of breaking the disulfide bridges (- S - S -) of mucopolysaccharide fibers, thereby loosening bronchial secretions.
+ The drug can disrupt the mucous barrier that protects the stomach lining, so it should be used with caution in people with a history of stomach or duodenal disease.
Assign
+ As an expectorant in respiratory diseases with thick phlegm such as acute bronchitis, chronic bronchitis...
+ Routine cleaning in tracheostomy.
+ Used to detoxify paracetamol overdose.
– Contraindications : history of asthma (due to risk of causing bronchospasm), use with antitussive drugs and bronchial secretion reducers.
How to use and dosage
Adults take 200mg/time, 3 times a day. Children take 200 - 400mg/day divided into 2 times depending on age.
Inhale 3 - 5 ml of 20% solution, 3 - 4 times a day
Instill 1-2 ml of 10-20% solution directly into the trachea once an hour to clean the trachea.
Note: due to its rapid action, it may cause fluid to overflow into the trachea if the patient is unable to cough to expel phlegm in time.
Tablets 200mg Powder Packet 200mg
Oral inhalation, tracheal instillation and oral solution 10%, 20%
1.2.2.2. Carbocysteine
BD: flemex, fluditex 2%, 5%, mucosan, solmux, phinathiol, rhinathiol…
– Effects, indications and contraindications: similar to acetylcysteine.
- Usage and dosage: adults take 4-6 tablets per day, divided into 2-3 times or 3 tablespoons of syrup per day, divided into 3 times. Children under 5 years old take 2 times per day, 1/2 teaspoon each time. Children
> 5 years old: take 1 teaspoon 3 times a day.
Capsule 375mg
Syrup 250mg/5ml (for adults) and 100mg/5ml (for children)
1.2.2.3. Diacetylcysteine
BD: mucothiol
Effects, indications and contraindications: similar to acetylcysteine.
Dosage: Adults and children > 7 years old take 600mg/day divided into 3 times, children 2-7 years old take 400mg/day divided into 2 times
Powder pack 150mg Tablets 200mg
1.2.2.4. Ambroxol
BD: Ambril, ambro, muxol. halixol, mucosolvan, mucolyse…
Is a metabolite of Bromhexine, effects, indications and contraindications are similar to brohexine
Adults and children > 10 years old take 30mg/time, 3 times a day, then 2 times a day if used for a long time.
Children 5 - 10 years old take 15mg/time, 3 times a day, if used for a long time, 2 times a day. 30mg tablets
Oral solution 30ml/5ml bottle Injection 2ml = 15mg
1.2.2.5. Bromhexine
It is a synthetic drug from the active pharmaceutical ingredient vasicine.
BD: bidivon, bisolvon, bixovom, broma, disolvon, mucine, paxirasol…
– Effect
+ Hydrolysis of mucoproteins leads to depolarization of mucopolysaccharides, breaking these high molecular fibers, modulating the activity of mucus-secreting cells. The result is a change in the structure and reduction in the viscosity of mucus, so mucus (phlegm) is easily expelled by the cough reflex.
+ Increases the penetration of antibiotics into bronchial secretions (amoxicillin, cefuroxime, erythromycin...)
– Indications and contraindications : similar to acetylcysteine
Usage and dosage
+ Adults and children > 10 years old take 8 mg once, 3 times a day or 3 tablespoons/day divided into 3 times. Children 5 - 10 years old take 4 mg/time. Children 2 - 5 years old take 2 mg/time.
+ Intramuscular or intravenous injection is only used in severe cases such as decreased mucus production and transport after surgical intervention. Slow intravenous injection dose (2 - 3 minutes) 4 mg, 2 - 3 times a day.
Tablets or sugar coated 4mg, 8 mg 2ml syringe = 4mg
60ml, 150ml oral solution bottle containing 120mg and 300mg
1.2.2.6. Epeprazinone