Test 2
Test 2
Test 2
PHARMACOLOGY
DMD2003
LECTURE #6
GASTROINTESTINAL (GIT)
PHARMACOLOGY
Anishka Lewis
objectives
■ Known as GI protectants
■ Includes;
– Sucralfate
– Bismuth Subsalicylate
– Prostaglandins (Misoprostol)
sucralfate
■ MOA
■ In pH < 4, sucralfate is
polymerised to form a sticky,
viscid yellow white gel which
adheres to ulcer base,
protecting the site against
acid, pepsin and bile salts.
■ Pharmacokinetics:
– Given orally, rapidly absorbed from the GIT, metabolized in the liver
and excreted in the urine.
■ Adverse Effects:
– Diarrhoea, Muscle cramps, nausea, vomiting, constipation
Anticholinergic agents
■ Includes Dicyclomine and Atropine
■ NOTE: Seldom used for PUD due to them being less effective
when compared to H2 antagonist and PPI
Antibiotic ulcer therapy
■ Combination must be used.
GASTROINTESTINAL
PHARMACOLOGY 2
EMETICS, LAXATIVES AND
ANTIDIARRHEAL AGENTS
Anishka Lewis
objectives
■ Upon completion of this Lecture, Students should have an
understanding of:
■ Deep breathing proceeds the actual vomiting to protect the lungs from
aspiration.
■ The pressure within the abdomen rises and the pressure within the chest
or thorax is lowered. The abdominal muscles contract to expel the
contents of the stomach.
■ The bile and acids from your stomach coming through your mouth to be
expelled can cause damage to your teeth, gums, and throat. It’s important
to take proper care of your mouth, even when you’re not feeling very
well. After you vomit, rinse your mouth with water, and then use a
mouthwash with fluoride.
■ Be aware that brushing your teeth immediately after vomiting can cause
additional problems. Stomach acid weakens the enamel on your teeth, so
brushing them right away can cause the enamel to erode. After you have
stopped throwing up, make sure to brush your teeth with toothpaste that
contains fluoride.
Vomiting and oral health
■ Types of constipation:
■ Side Effects: oil leakage into anal sphincter, long term use interfere
with absorption of fat –soluble vitamin.
Osmotic laxatives
■ Solutes that are not absorbed in the intestine.
■ Approaches in treatment:
– Replacement fluid and electrolytes
– Treatment of cause
– Antidiarrhoeal agents
Fluid and electrolyte
replacement
■ ORAL REHYDRATION SALTS (eg. Pedialyte®), Usually the only
therapy needed for acute diarrhea (body defense mechanism).
■ ANTIMUSCARINIC DRUGS:
– Atropine
– Hyoscine
– Dicyclomine
■ OPIATE-LIKE DRUGS
– Diphenoxylate (Lomotil)
– Loperamide
■ OPIATE-LIKE DRUGS
■ Greater potency than morphine: Diphenoxylate (2 x)
Loperamide (40-50 x)
■ Limited entry into CNS, therefore activity only on peripheral opiate
receptors
■ MEBEVERINE
– Activity only on GIT (no activity on other smooth muscles).
– Direct relaxant action on smooth muscles.
■ Bacterial infections:
AUTOCOIDS, INFLAMMATION,
ALLERGY &
IMMUNOMODULATORS
Anishka Lewis
Objectives
2. Local hormones
■ Histamine
■ 5-hydroxytryptamine (Serotonin/5-HT)
■ Angiotensin
■ Prostaglandins
■ Leukotrienes
histamine
Histamine synthesis & metabolism
• A biogenic amine formed in
many tissues.
Effects in Inflammation
■ Vasodilation and increased vascular permeability : 5HT
released from platelets and causes vasodilation by acting on
5HT1 receptors on the endothelial cells → NO release→
relaxation
Clinical uses of 5-ht
AGONIST ANTAGONIST
■ 5-HT1D – sumatriptan – Used in ■ 5-HT2 - dihydroergotamine,
ketotifen, pizotifen, methysergide,
migraine therapy cyproheptadine, ketanserin
– A high specificity for these receptors
on the cranial blood vessels
– Used to treat migraine
– Decrease activity of trigeminal nerve headache
(useful in treating cluster headaches).
■ 5-HT3 – ondansetron,
■ 5-HT4 – metoclopramide, cisapride granisetron, tropisetron
– Used to treat GIT disorders e.g.
gastric reflux – Used to suppress nausea and
vomiting (anti-emetic effect
angiotensins
angiotensins
■ Nerves: it increases the sensation of thirst, the desire for salt, encourages the release
of other hormones that are involved in fluid retention.
■ The kidneys: it increases sodium retention and alters the way the kidneys filter
blood. This increases water reabsorption in the kidney to increase blood volume and
blood pressure.
Angiotensin
■ Inhibitors of ACE and blockers of angiotensin II receptors
are now used in the treatment of hypertension, congestive heart
failure and other conditions that are due to excess of
angiotensin II activity
Eicosanoids
eicosanoids
■ Can be classified as:
■ Prostaglandins (PGs)
■ Thromboxanes (TXs)
■ Leukotrienes (LTs)
■ Bronchospasm
RESPIRATORY
PHARMACOLOGY
ANISHKA LEWIS
objectives
■ Upon completion of this Lecture, students should be able to:
■ Corticosteroids
– Prednisone, Prednisolone, Beclomethasone diphosphate
Sympathomimetic drugs
■ Selective beta-2 agonists are primary bronchodilators.
■ Relieves bronchospasm
■ Includes:
– Short acting β2 agonists
■ Salbutamol (Albuterol) and Terbutaline
– Longer acting β2 agonists
■ Salmeterol, Formoterol, Fenoterol, Bambuterol &
Pirbuterol
Sympathomimetic drugs
MOA:
■ Anti-inflammatory drugs.
■ Inhaled steroids
■ PHARMACOKINETICS
– It is given orally. Beneficial effects are seen after 6-12 weeks of
use.
– It is used for the prophylaxis of bronchial asthma and other
allergic disorders like allergic rhinitis
■ ADVERSE EFFECTS
– Drowsiness, dry mouth, dizziness and weight gain
Bronchial asthma and dentistry
1. A small amount of water or dental materials used in dental procedures
may aspirate into the respiratory passage and trigger an acute attack of
bronchial asthma. Salbutamol inhalation should be given immediately.
The dental procedure may be continued after the patient recovers.
CARDIOVASCULAR
PHARMACOLOGY
ANISHKA LEWIS
objective
CHAMBERS CIRCULATION
■ Hypertension
■ Angina
■ Heart failure
■ Arrhythmia
antihypertensive
Control of blood pressure
■ The pressure in the CVS is determined by 3 elements.
– Heart Rate
WHAT IS HYPERTENSION?
hypertension
4. Sympatholytics
6. Vasodilators
Diuretics
■ Mild antihypertensive effects
■ Classes:
– Loop diuretics
– Thiazide diuretics
2. Ganglion blockers
✔ Trimethaphan
■ Three Types
1. Stable Angina
2. Unstable Angina
3. Variant Angina
angina
■ BETA BLOCKERS
■ Useful in Variant angina since they dilate the coronaries and relieve
vasospasm.
■ This occurs when the heart muscle has suffered an injury and
cannot keep up its work.
– Cardiac Glycosides
Cardiac glycosides (CGS)
■ MOA:
Potent inhibitors of cellular Na+/K+ ATPase. Usually this
system moves sodium ions out of the cell and potassium into
the cell. CGs results in increased intracellular Na+. The
Na+/Ca++ exchanger compensates by removing Na+ from the
cells and increasing the entry of Ca++ into the cells. An
increase in Ca++ results in an increase in the contractility of
the heart.
Cardiac glycosides
ADVERSE EFFECTS DENTAL DRUG
INTERACTION
■ Anorexia, nausea, vomiting ■ Sympathomimetics
(epinephrine) added to local
■ Headache, drowsiness, visual anaesthetics should be used
disturbances, with caution.
■ Sympathomimetics can
■ Arrhythmias– if a sufficient over dose increase the chance of
is given. arrhythmias occurring with
CGs.
■ Increased salivation, increase in
gagging reflex
ARRHYTHMIAS (DYSRHYTHMIAS)
■ A cardiac arrhythmia is any abnormal heart rate or rhythm.
■ Factors affecting heart rhythms:
– Coronary artery disease.
– Electrolyte imbalances in your blood (such as sodium or
potassium).
– Changes in your heart muscle.
– Injury from a heart attack.
– Irregular heart rhythms can also occur in "normal, healthy"
hearts.
Vaughan-Williams classification
of antiarrhythmic drugs
SODIUM CHANNEL BLOCKERS
■ MOA: Binds to and block the fast sodium channels that are
responsible for the rapid depolarization (phase 0) of fast-response
cardiac action potentials.
■ DENTAL IMPLICATION:
– Xerostomia