It describes the action of Anticholinergics on the genitourinary system. Detailed description of each anticholinergic drug is given .
they can be given in urinary incontinence.
2. INTRODUCTION
• An anticholinergic agent is a substance that blocks
the neurotransmitter acetylcholine in the central and the peripheral
nervous system.
• These agents inhibit parasympathetic nerve impulses by selectively
blocking the binding of the neurotransmitter acetylcholine to its receptor
in nerve cells.
• The nerve fibers of the parasympathetic system are responsible for the
involuntary movement of smooth muscles present in the gastrointestinal
tract, urinary tract, lungs, and many other parts of the body.
5. UNDERSTANDING THE NEED TO ADMINISTER
ANTICHOLINERGICS
If you urinate often and have leaks between bathroom visits, you may have
signs of an overactive bladder (OAB). According to the Mayo Clinic, OAB may
cause you to urinate at least eight times in a 24-hour period. If you wake up
often in the middle of the night to use the bathroom, OAB may be the
cause.
Anticholinergic drugs are often prescribed to treat OAB.
These drugs work by relaxing your bladder muscles.
They also help prevent urine leaks by controlling bladder
spasms.
Most of these drugs come as oral tablets or capsules.
10. Introduction
• Atropine, a naturally occurring belladonna alkaloid
• Atropine Sulfate Injection, USP is a sterile,
nonpyrogenic isotonic solution of atropine sulfate
monohydrate in water for injection with sodium chloride
sufficient to render the solution isotonic. It is administered
parenterally
by subcutaneous, intramuscular or intravenous injection
11. Uses
• Atropine is also employed to reduce
hypermobility states of the urinary bladder. It is
still occasionally used in enuresis (involuntary
voiding of urine)
• As an antidote to cholinergic
• To suppress rigidity and tremors in parkinsonism
• It causes vasodilation
• Cystitis
• Uretheritis
12. • Dosage-
Systemic –Adults- 0.4-0.6mg every 4-6 hour
Children-0.01-02mg/kg
Contraindications-
Atropine is a highly potent drug and due care is essential to
avoid overdosage, especially with intravenous
administration. Children are more susceptible than adults
to the toxic effects of anticholinergic agents. Not to be
taken by thyroid patients ,UC patients.
Pharmacokinetics
Significant levels are achieved in the CNS within 30 minutes
to 1 hour and disappears rapidly from the blood with a half-
life of 2 hours. About 60% is excreted unchanged in the
urine, most of the rest appears in urine as hydrolysis and
conjugation products.
13. DRUG INTERACTIONS
• This medication can cause dizziness ,
drowsiness, or blurred vision.
• Interact with bronchodilators, digoxin, bladder
or urinary medications such as
detrol,oxybutynin
14. • Side effects-
• Dryness of the mouth,
• blurred vision,
• photophobia
• tachycardia
• Anhidrosis
• tremor,
• fatigue
• ataxia.
17. INTRODUCTION
• Oxybutynin (brand names Ditropan, Lyrinel
XL, Lenditro , Driptane , Uripan (Middle East) is
an anticholinergic medication used to relieve urinary
and bladder difficulties, including frequent urination
and inability to control urination (urge incontinence),
by decreasing muscle spasms of the bladder.
18. USES
• Oxybutynin reduces muscle spasms of the bladder
and urinary tract.
• Oxybutynin is used to treat symptoms of overactive
bladder, such as frequent or urgent urination,
incontinence (urine leakage), and increased night-
time urination.
19. Dosage
• Initial:
Immediate release tablet or Syrups: 5 mg 2 to 3 times daily.
Extended release tablets: 5 mg once daily.
• Usual Pediatric Dose for Urinary Incontinence:
• Immediate Release:
Greater than 1 to 5 years: 0.2 mg/kg per dose, 2 to 4 times
daily.
Greater than 5 years: 5 mg 2 times daily, up to 5 mg 3 times
daily.
20. Oxybutynin is rapidly absorbed achieving
Cmax within an hour, following which plasma
concentration decreases with an effective half-life
of approximately 2 to 3 hours. The absolute
bioavailability of Oxybutynin is reported to be
about 6%
Metabolized mostly in the liver and gut wall.
excreted unchanged in the urine
21. If you are taking this drug with other
medications such as benadryl ,you will
experience other side effects also.
Combining pramlintide with oxybutynin
should be avoided.
Oxybutynin may also delay passage of
potassium tablets through the digestive
system.
22. SIDE EFFECTS
Acid or sour stomach
belching
decreased sweating
diarrhea
difficulty having a bowel movement (stool)
drowsiness
dryness of the eyes, mouth, nose, or throat
heartburn
indigestion
runny nose
stomach discomfort, upset, or pain
25. DOSAGE
Initial dose: 5 mg orally once daily
Maintenance dose: 5 to 10 mg orally once
daily
Combination regimen: 5 mg PO qDay in
combination with mirabegron 25 mg PO qDay
Not to be given in pediatric patient
26. Solifenacin ( trade name Vesicare) is a medicine of
the antimuscarinic class and was developed for treating
contraction of overactive bladder with associated problems
such as increased urination frequency and urge incontinence
27. DITROPAN® (oxybutynin chloride) is
contraindicated in patients with urinary
retention, gastric retention and other severe
decreased gastrointestinal motility
conditions, uncontrolled narrow-
angle glaucomaand in patients who are at risk
for these conditions.
28. Some products that may interact with this
product may include :
Pramlintide, potassium tablets , and certain
antifungals.
29. Solifenacin is used to treat an overactive bladder. By relaxing
the muscles in the bladder, solifenacin improves your ability
to control your urination. It helps to reduce leaking of urine,
feelings of needing to urinate right away, and frequent trips to
the bathroom.
30. PHARMACOKINETICS
Peak plasma concentrations are reached 3 to 8 hours after
absorption from the gut. In the bloodstream, 98% of the substance
are bound to plasma proteins, mainly acidic ones. Metabolism is
mediated by the liver enzyme , the metabolism of solifenacin is
impaired, leading to an increase in its concentration in the body and
a reduction in its excretion
CONTRAINDICATIONS
Solifenacin is contraindicated for people with urinary retention,
gastric retention, uncontrolled or poorly controlled closed-
angle glaucoma, severe liver disease and hemodialysis.
SIDE EFFECTS
side effects of solifenacin are dry mouth, blurred vision, and
constipation. As all anticholinergics, solifenacin may rarely
cause hyperthermia due to decreased perspiration. Overdose may
cause arrhythmias .
32. Imipramine, sold under the brand name Tofranil among
others, is also a a tricyclic antidepressant (TCA)
It works by restoring the balance of certain natural
substances (neurotransmitters such as norepinephrine) in
the brain. For bed-wetting, this medication may work by
blocking the effect of a certain natural substance
(acetylcholine) on the bladder
33. DOSAGE:
TABLETS -Initial dose: 100 mg orally once a day, increasing to 200
mg/day if necessary
-Titration dose: After increasing the dose to 200 mg/day, if there is
no response after 2 weeks, increase the dose to 250 to 300 mg/day.
CHILDREN:
25mg/OD in the evening
Do not stop giving imipramine suddenly, as your child may get
withdrawal symptoms.
34. Major depressive disorder (MDD)
Bedwetting in children (Enuresis)
Bulimia nervosa
Panic disorders
Neuropathic pain
35. The drug is contraindicated during the acute recovery period after a myocardial infarction.
The use of monoamine oxidase inhibiting compounds is contraindicated. Hyperpyretic crises
or severe convulsive seizures may occur in patients receiving such combinations.
Pharmacokinetics
Rapidly and well absorbed (>95%) after oral administration . The
primary site of absorption is the small intestine .
- Imipramine is 60-96% bound to plasma proteins in circulation,
exclusively metabolized by the liver
- primarily excreted in the urine with less than 5% present as the
parent compound
36. dry mucous membranes,
blurred vision,
increased intraocular pressure,
hyperthermia,
constipation
adynamic ileus,
urinary retention,
delayed micturition,
dilation of the urinary tract
OVERDOSAGE MAY EVEN RESULT IN DEATH
39. Define Anticholinergics and give its
classification.
What are the indications of giving atropine.
State the common side effects of
anticholinergics.
40. Essentials of medical pharmacology
By- KD Tripathi
Textbook of pharmacology
By – Suresh K. Sharma
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