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Pharmacology > Cholinolytic drugs > Flashcards

Cholinolytic drugs Flashcards

1
Q

What are cholinolytics?

A

They are drugs blocking cholinoreceptors and preventing the development of acetylcholine actions.

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2
Q

What are the different types of cholinolytics?

A

M and N

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3
Q

What are the M cholinolytics?

A
  1. Natural alkaloids
    - Atropine sulfate
    - Hyoscine or scopolamine hydrochloride
  2. semisynthetic cholinoblockers- Ipratropium bromide
  3. synthetic cholinolytics
    - pirenzepine
    - tropicamide
    - darifenacin and solifenacin
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4
Q

what are the pharmacodynamics of atropine?

A
  • It blocks all receptors but they possess different sensitivity towards it
  • it inhibits functions that are strongly under the influence of parasympathetic nervous system
  • In low doses it inhibits the exocrine gland secretion
  • intermediate doses lead to ocular effects and tachycardia
  • higher doses lead to relaxation of smooth muscles
  • the highest doses lead to inhibition of parietal cell secretion
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5
Q

what are the pharmacological effects of atropine on the central nervous system?

A
  • In therapeutic dose it leads to slight stimulation of respiratory and vagal centres
  • in toxic doses stimulation of brain becomes more prominent at which there is hyperactivation, irritation, hallucination, and deliriums
  • in higher doses inhibition follows stimulation leading to lethal outcome
  • it has an anti tremor activity and decreases motor disturbances in Parkinson’s disease
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6
Q

Why is atropine not used for Parkinson’s disease nowadays?

A

It has non selective blockage of muscarinic receptors at which it exerts different peripheral effects hence it isn’t used for Parkinson’s and instant benztropine and biperiden.

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7
Q

What are the pharmacological effects of atropine on the cardiovascular system?

A
  • Therapeutic doses block the M2 receptors of sinus node preventing the inhibitory action of the vagus nerve on the heart and causes and significant tachycardia
  • increase of AV conductivity and increase in heart oxygen demand
  • in toxic doses it causes block of ventricular conductivity hence atrial and ventricular trembling is developed
  • in normal and toxic doses it causes dilation of skin vessels of the upper part of the body and that’s due to the compensatory activation of body heart irradiation through convection
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8
Q

what are the pharmacological effects of atropine on the respiratory system?

A

It causes relaxation of the upper respiratory tract muscles and inhibition of the secretion function of bronchi at which it prevents reflector bronchospasm and general anesthesia

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9
Q

what are the pharmacological effects of atropine on the GIT?

A
  • It inhibits the motor activity of GIT and secrete your function however the activity of these organs isn’t completely abolished because they’re regulated by local hormones and non cholinergic intramural neurons
  • decreases salivation resulting into the dryness of mouth and difficulties in swallowing and speaking
  • it significantly decreases the secretory activity of the pancreas and intestine glands
  • Secretion of violence and changed because it isn’t under the influence of cholinergic system
  • it decreases the tone of the intestine gallbladder, biliary ducts, stomach
  • it inhibits peristalsis and causes Constipation
  • it eliminates diarrhea caused by M cholinomimetics and anticholinesterase drugs
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10
Q

what are the pharmacological effects of atropine on the urogenital tract?

A

It relaxes smooth most soles of the urinary bladder and causes urine retention and it has no significant effect on the uterus

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11
Q

what are the pharmacological effects of atropine on exocrine glands?

A

Sweating is decreased causing dry skin and hot skin which can increase body temperature

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12
Q

what are the local pharmacological effects of atropine on the eye?

A
  1. Mydriasis by the blockage of circular muscle of the pupil for seven to 10 days
  2. Photophobia
  3. Cycloplegia for 8 to 12 days
  4. increase in intraocular pressure
  5. secretion of lacrimal glands is inhibited at which eye dryness is present
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13
Q

describe the pharmacokinetics of atropine.

A
  • It is absorbed from GIT and other biological membranes
  • it has a big volume of distribution
  • it crosses the BBB
  • it’s half life is 2 hours
  • 60% of it is excreted in unchanged form while the rest is exposed to hydrolysis and conjugation
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14
Q

what are the indications of atropine?

A
  1. It is used as spasmolytic in GIT problems
  2. it is used as a premedication and general anesthesia to prevent muscarinic effects like laryngospasm, hypersalivation, bronchospasm, and heart arrest
  3. it is used in cases of acute symptomatic bradycardia
  4. it is used in intoxications by anticholinesterases
  5. it is used as an antitoxin and fungal intoxications
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15
Q

How do we treat intoxication of atropine?

A
  1. Washing of the stomach, administration of activated carbon, and forced diuresis
  2. decrease of body temperature by cooling or wet covering
  3. Putting the patient in a dark room to decrease photophobia
  4. the use of acetylcholinesterase reversible inhibitors as a specific treatment which can penetrate through BBB
  5. anxiolytics are used to remove excitation
  6. beta adrenal blockers are used to remove express tachycardia
  7. artificial respiration
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16
Q

what is the differences between scopolamine and atropine?

A
  • Its pharmacological effects are similar to atropine but in contrast it inhibits the CNS
  • its anti vomiting activity is more prominent at which it inhibits the trigger zone and is useful in sea diseases
  • it has an amnestic and sedative hypnotic effects
  • its effect on the eye and exocrine gland is more prominent compared to atropine
17
Q

what are the indications of scopolamine?

A
  1. Prevention of air and sea sickness
  2. Premedication
  3. spasm of smooth muscles and inner organs
18
Q

What is the mechanism of action of ipratropium bromide?

A

It blocks all types of umm receptors and inhibits them leading to the decrease in release of acetylcholine and it has no effect on CNS

19
Q

describe the pharmacokinetics of ipratropium bromide.

A

Parenteral administration leads to bronchodilation tachycardia and inhibition of glandular secretion and when it is used as an inhalation way its effects are limited only by action on the upper respiratory ways

20
Q

what is the common side effect of ipratropium bromide?

A

Dryness of mouth

21
Q

what are the uses of ipratropium bromide?

A

It is used as an aerosol or solution for the treatment of bronchial asthma and pulmonary obstructive disease at which its effect lasts four to six hours

22
Q

what is the mechanism of action of pirenzepine?

A
  • It has high affinity to M1 and M4 receptors compared to M2 and M3 receptors
  • it has selective antimuscarinic effect and does inhibit the secretion of HCL and pepsinogen even in small doses and does improve the blood supply of stomach.
23
Q

What are the uses of pirenzepine?

A

it is used for a complex treatment of peptic ulcers

24
Q

how do darifenacin and solifenacin act?

A

They block muscarinic receptors of the urinary bladder and increase the volume of the urinary bladder and they do have high affinity towards M3 receptors which decrease the systemic side effect of them

25
Q

how are darifenacin and solifenacin used?

A

They’re mainly used to treat overactive urinary bladder

26
Q

what are the usages of tropicamide?

A

It is used as eye drops for mydriasis and cycloplegia

27
Q

what are the side effects of M cholinolytics?

A
  1. Dryness of mouth
  2. Cycloplegia
  3. Tachycardia
  4. Constipation
  5. urine retention
  6. allergic reactions like dermatitis, conjunctivitis, or edema of the eyelids

Pharmacology (11 decks)

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