Agents affecting digestive

organs function
 Among substances that influence on
functioning of digestive organs there are
following groups of drugs:
Drugs effecting appetite;
Emetic and antiemetic drugs;
Drugs which are used in case of disturbed function of
gastric glands;
Drugs effecting liver function;
Drugs used in case of disturbed excretory function of
pancreas;
Laxative agents;
Drugs which influence on motor function of intestine
 Drugs which
influence on
appetite:
Drugs which Drugs which
improve depress
appetite appetite
 Anorexia, scrawny

Fast, depression, diseases

Common wormwood
Artemisia absinthium
Centaury
Centaurium
Milfoil
Achillea millefolium

Plants with bitter taste

Adiposities
 Drugs which depress
appetite (anorexigenic drugs)

Decreases the activity

of central links of appetite
reflex via increasing the
activity of some structures
of CNS
for alimentary and endocrine
obesity as additional therapy
can cause insomnia,
excitement, increasing of AP,
Phepranonum slight dependence
0,025 g tablets
 Emetic drugs
Apomorphini hydrochloridum

stimulates D2 dopamine receptors of

trigger zone of vomiting center
for acute poisonings with food products,
chemical substances, drugs etc.
used subcutaneously 0,2-0,5 ml 1 %
solution
Provoking the vomiting is contraindicated

For unconscious patients

During pregnancy
For senile persons
For acute poisons caused volatile or
corrosive toxins
For patients with ulcer disease
For acute poisons caused neuroleptics
etc.
 antiemetic drugs
Metoclopramide (reglan, cerucal) – blocks D2
dopamine and 5-HT3 serotonin receptors of trigger zone of
vomiting center, increases motor activity of stomach and
intestine
Aethaperazinum - blocks D2 dopamine receptors,
for vomiting of central origin (uremia, after surgical
operations, radial disease, vomiting caused by anticancer
drugs, acute intoxication with cardiac glycosides).
Contraindicated during pregnancy.
Scopolaminum (Aeronum), antihistamines (Dimedrol,
Diprasin) – depress cerebella (M-cholinoreceptors and
H1-histaminoreceptors) and vomiting center, for sea-
sickness and other disorders of vestibular apparatus
 Metoclopramide (reglan, cerucal)
0,01 g tablets, ampoules 2 ml of 0,5 % solution
 Motilium (Domperidonum)

D2 dopamine receptors
antagonist
doesn’t cross HEB,
doesn’t cause Parkinson
syndrome (as
neuroleptics do)
for hypotonia of stomach,
reflux-oesophagitis

0,01 g tablets
Drugs which stimulate gastric
secretion

With diagnostic aim: caffeine, histamine,

gastrin

With treating aim: plantain juice,

Plantaglucide, natural gastric juice, pepsin,
hydrochloric acid
Plantain herb
 Drugs which depress gastric secretion
Drugs which block choline receptros:
M-cholinoblockers (nonselective): atropine sulfate
M1-cholinoblockers with selective action: gastrozepin
ganglionblockers: pirilen, benzohexonium
Drugs which block histamine-Н2-receptors: cimetidine,
ranitidine, famotidine, nizatidine, roxatidine
Inhibitors of proton pump: omeprazole, controlok
Prostaglandines and their synthetic derivatives: misoprostol
Antacids:
with systemic action: sodium hydrocarbonate
without systemic action: aluminum hydroxide, magnesium
oxide, almagel, maalox, renni
Gastroprotectors:
Drugs which form protective membrane and mechanically
protect mucous membrane of stomach: sucralfate, de-nol
Drugs which increase protective function of mucous
barrier and stability of mucous membrane towards action
of damaging factor: carbenoxolon, misoprostol
Atropine sulfate (Atropini sulfas)
Gastrozepin (Gastrocepinum)
Cimetidine
0, 2 g tablets
0,15 g and 0,3 g tablets and ampoules with 2 ml of
2,5 % solution
 Famotidin
0,02 g and 0,04 g tablets
Omeprazole
0,02 g capsules
 Antacides

with systemic without systemic

action action
 Almagel
Combined drug which contains gel of aluminum hydroxide, magnesium oxide and D-sorbit
170 ml bottles
Antacides
 Maalox
Combined drug which contains gel of aluminum hydroxide and
magnesium oxide
Sucralfate

forms glue in acid condition

of stomach which covers the
surface of ulcer
does not act on normal
mucous
for ulcer disease
duration of action 6 hr
before meal
hasn’t be combined with
antacids (Al-containing) and
H2 –
histaminoblockers (brake – 2
hours)
 De-nol (bismuthi subcitras)
binds to glycoproteins of gastric mucous, especially to
necrotic masses of ulcer surface, forms protective layer
Schemes of combined treatment of
ulcer disease

De-nol + amoxycillin
De-nol + metronidazole
Omeprazole + amoxycillin + clarythromycin
De-nol + clarythromycin + metronidazole
De-nol + controlok (pantoprazol) + amoxycilin +
clarythromycin
 Pylobact
Omeprazole + Clarythromycin + Tinidazole
 Other substances effecting
digestive organs function :

Drugs effecting liver function;

Drugs used for disturbed excretory
function of pancreas;
Laxatives;
Drugs effecting motor function of
intestine
Hepatotropic
drugs
Drugs which increase
bile quantity and bile flux

Liver protectors

Cholelytholytics
 Drugs effecting bile formation and bile flux

Drugs which stimulate bile production (choleretics,

cholesecretics)
Drugs which increase secretion of bile and stimulate production of
bile acids (real choleretics)
а) drugs which contain bile acids (allochol, cholenzyme)
б) synthetic drugs (nicodine, oxafenamide)
в) drugs of plant origin (common immortelle, stigma of corn,
pepper mint, tansy, dog-rose)

Drugs which increase secretion of bile primarily due to water

component (hydrocholeretics: mineral waters, valerian drugs)

Drugs which stimulate bile flux (cholekinetics)

drugs which cause increasing of gall-bladder tone and decreasing
of bile ducts tone (cholekinetics: magnesium sulfate, sorbit, barberries).
drugs which cause relaxation of bile ducts tone (cholespasmolytics:
M-cholinoblockers, euphyllin, nitroglycerine)
Stigma of corn

Common immortelle
Dog-rose

Choleretics of plant origin

 Pharmacodynamics of magnesium
sulfate depending on route of its
administration

orally – laxative action

i. m., i. v. – hypotensive, antiarrhythmic,
antiseizures action
i. v. – very slowly, dropply (when used i. v.
quickly - can depress respiratory center and
course respiratory arrest, specific antagonist
– calcium chloride i. v.)
Clinical classification of antioxidants which may
be used as hepatic protectors

Antioxidants of direct action

Drugs which contain vitamin E (tocopherole acetate, aevit)
Vitamin C drugs (ascorbic acid, galascorbin, ascorutin)
Bioflavonoids (legalon, flamin, flakumin, sylibor, convaflavin )
Drugs which include sulfhydril groups (unithiol, thiosulfate
sodium)

Antioxidants of indirect action

Drugs which regulate phospholipid contents of cell membranes
(essentiale, lipin, retinol, aevit)
Precursors of pyridine nucleotides (nicotinic acid, nocotinamid )
Precursors of glutation (metionin, cystein, glutamic acid )
Drugs which induct glutationperoxydase (selenium containing
drugs)
Other drugs which increase antioxidant potential of blood and
tissues (lipoic acid, lipamid, organic drugs of liver )
 Tocopherole acetate (Tocopheroli acetas)
Vitamin E is produced in many forms: 5 %, 10 % and 30 % oil solution in 10, 20 and 50 ml
bottles; elastic capsules with 0,1 and 0,2 ml of 50 % solution in oil; ampoules with 1 ml of 5
%, 10 % and 30 % oil solutions.
Saint-Mary thistle (milk thistle)
Carsil Legalon
 Essentiale
5 ml ampoules and capsules
Pancreatin (Panсreatinum) – enzymes of pancreas
Panzynorm forte
Festal, Enzistal, Penzital
Mezym-forte
No-spa, nicospan
Baralgin
Purging buckthorn (bark)
 Bisacodil
suppositories – onset 1-2 hr, for chronic constipation
Guttalax (Natrii picosulfas) – after activating in column under the influence
of bacterial sulfatase irritates mucous of intestine, onset – 10-12 hr, for
chronic constipation
Just because laxatives are
available without a
prescription doesn't mean
that they're without risk.

Warning: Use of stimulant

laxatives over a long
period may lead to
dependence and might
permanently damage
intestine and colon
Important: Laxatives are intended for short-term use,
generally less than 1 week.

Side effects of laxatives:

Prevention of vitamin and mineral absorption
Imbalance of electrolyte household
Cascara and senna commonly cause yellow-brown
urine
bloody stools, severe cramping, pain, weakness,
dizziness, unusual tiredness, rectal bleeding
diarrhea, nausea, vomiting, irritation, stomach
cramping
 Natural laxatives
Avocado
Dandelion greens
Dried apricots
 Natural laxatives
Figs
Flaxseed
Mango
 Natural laxatives
Prunes
Rhubarb
Prunes and prune juice
Contain high concentrations
of simple sugars, which are
known as sorbitol. These
simple sugars cannot be
digested, causing intestines
to flood with fluid, softening
stools and moving bowels.
One cup of prunes contains
12 grams of fiber, which will
help get gut system going
even faster than the juice
alone. Prunes also contain
dihydrophenylsatin, a
natural laxative agent.
 Natural laxatives
cabbage, carrot, beetroot
Bilberry Saint-John’s-wort
Pepper mint Matricary
Imodium – for noninfectious diarrhea
H2 Antagonists (Cimetidine, Ranitidine, Famotidine)
• Mechanisms of action:
–– Suppress secretory responses to food stimulation and nocturnal
secretion of gastric acid via their ability to decrease (indirectly) the
activity of the proton pump.
–– Also partially antagonize HCl secretion caused by vagally or
gastrininduced
release of histamine from ECL-like cells (GI mast cells)
–– No effects on gastric emptying time
• Uses:
–– PUD (overall less effective than proton pump inhibitors)
–– Gastroesophageal reflux disease (GERD)
–– Zollinger-Ellison syndrome
• Side effects:
–– Cimetidine is a major inhibitor of P450 isoforms → drug interaction
via ↑ effects
–– Cimetidine →↓ androgens → gynecomastia and ↓ libido
 Proton Pump Inhibitors

• Mechanism of action:

–– Omeprazole and related “–prazoles” are irreversible, direct

inhibitors
of the proton pump (K+/H+ antiport) in the gastric parietal cell
• Uses:
–– More effective than H2 blockers in peptic ulcer disease (PUD)
–– Also effective in GERD and Zollinger-Ellison syndrome
–– Eradication regimen for H. pylori
Misoprostol
• Mechanism of action: PGE1 analog, which is cytoprotective →↑
mucus
and bicarbonate secretion and ↓ HCl secretion
• Uses: Previously for NSAID-induced ulcers, but PPIs are now used
Sucralfate
• Mechanism of action: polymerizes on gastrointestinal luminal surface
to form a protective gel-like coating of ulcer beds. Requires acid pH
(antacids may interfere)
• Uses: ↑ healing and ↓ ulcer recurrence
 Bismuth Subsalicylate
• Mechanism of action: like sucralfate, binds selectively
to ulcer, coating
it, and protecting it from acid and pepsin
• Combined with metronidazole and tetracycline to
eradicate H. pylori (BMT regimen)
Antacids: Al (OH)3, Mg (OH)2, CaCO3
• Mechanism of action: bases that neutralize protons in
the gut lumen
• Side effects: Constipation (Al+++), diarrhea (Mg++);
rebound hyperacidity
ANTIEMETICS
Antiemetic Mechanisms
The figure below shows the complexity of the emetic pathways with an impact
on the vomiting center and reveals the multiplicity of receptor types involved,
including those activated by ACh, DA, 5HT, histamine, and endogenous opiopeptides.
Drugs for Nausea and Vomiting
Drugs for nausea and vomiting include:
• 5HT3 (a serotonin receptor: see next chapter)
antagonists: ondansetron
(commonly used in cancer chemotherapy), granisetron
• DA antagonists: prochlorperazine, metoclopramide
(also used in
cancer chemotherapy; also prokinetic in GERD)
• H1 antagonists: diphenhydramine, meclizine,
promethazine
• Muscarinic antagonists: scopolamine
• Cannabinoids: dronabinol
• NK1-receptor antagonist: aprepitant (NK1 is a
receptor to substance P)