Pharm 236 Ch 20 Anticholinergic Drugs

Front 1

________________ drugs block the action of acetylocholine on the parasympathetic nervous system.

Back 1

Antichoinergic

Front 2

_________ amines are uncharged lipid soluble molecules

Back 2

Tertiary

Front 3

Some belladonna derivatives and synthetic anticholinergics are _______________ amines.

Back 3

Quatenary

Front 4

When given at high doses a few anticholinergic drugs are also able to block _________ receptors in autonomic ganglia and skeletal muscles.

Back 4

Nicotinic

Front 5

Because cholinergic ___________ receptors are widely distributed in the body anticholinergic drugs produce effects in a varity of locations including the CNS, heart, smooth muscle, glands and the eye.

Back 5

Muscarinic

Front 6

Prototype of anticholinergic drugs a naturally occurring belladonna alkaloid that can be extracted from the belladonna plant or prepared synthetically

Back 6

Atropine

Front 7

A belladonna alkaloid used in gastrointestinal and genitourinary disorders characterized by spasm increased secretion and increased motility.

Back 7

Hyoscyamine

Front 8

May be given by inhalation for bronchodilating effects.

Back 8

Ipratropium or tiotropium

Front 9

When given parenterally depresses the CNS and causes amnesia, drowsiness, euphoria, relaxation and sleep.

Back 9

Scopolamine

Front 10

A semisynthetic derivative of atropine used as eye drops to produce mydriasis and cycloplegia

Back 10

Homatropine hydrobromide

Front 11

Describe the characteristics of tertiary amines and give examples of two medications in this category.

Back 11

Most anticholinergic medications are either tertiary amines or quaternary amines. Tertiary amines are uncharged lipid soluble molecules. Atropine and scopolamine are tertiary amines and therefor are able to cross cell membranes readily. They are well absorbed from the gastrointestinal tract and conjunctiva, and they cross the blood brain barrier. Tertiary animes are excreted in the urine.

Front 12

Describe the characteristics of quaternary amines.

Back 12

Some belladonna derivatives and synthetic anticholinergics are quaternary amines. These drugs carry a positive charge and are lipid insoluble. Consequently, they do not readily cross cell membranes. They are poorly absorbed from the GI tract and do not cross the blood brain barrier. Quaternary amines are excreted largely in the feces.

Front 13

Describe the general characteristics of anticholinergic drugs.

Back 13

In general, anticholinergic drugs act by occupying receptor sites on target organs innervated by parasympathetic nervous system, thereby leaving fewer receptor sites free to respond to acetylcholine. Parasympathetic response is absent or decreased depending on the number of receptors blocked by anticholinergic drugs and the underlying degree of parasympathetic activity. Because cholinergic muscarinic receptors are widely distributed in the body anticholinergic muscarinic receptors are widely distributed in the body, anticholinergic drugs produce effects in a variety of locations, including the central nervous system, heart, smooth muscle, glands, and the eye.

Front 14

How do anticholinergic drugs affect the cardiovascular system?

Back 14

Anticholinergic drugs cause decreased cardiovascular response to the parasympathetic, vagal, stimulation that slows heart rate. Atropine is the anticholinergic drug most often used for its cardiovascular effects. According to ACLS, advanced cardiac life support protocol, atropine is the drug of choice to treat symptomatic sinus bradycardia. Low doses less than 0.5mg may produce a slight and temporary decrease in heart rate; however, moderate to large doses 0.5 to 1mg increase heart rate by blocking parasympathetic vagal stimulation. Although the increase in heart rate may be therapeutic in bradycardia it can be an adverse effect in patient with other types of heart disease because atropine increases the myocardial oxygen demand. Atropine usually has little or no effect on blood pressure. Large doses cause facial flushing because of dilation of blood vessels in the neck.

Front 15

How do anticholinergic drugs affect the respiratory system?

Back 15

Anticholinergic drugs cause bronchodilation and decreased respiratory tract secretions. Anticholinergics block the action of acetylcholine in bronchial smooth muscle when given by inhalation. this action reduces intracellular GMP a bronchoconstrictive substance. When anticholinergic drugs are given systemically, respiratory secretions decrease and may become viscous, resulting in mucous plugging of small respiratory passages. Administering the medications by inhalation decreases the effect while preserving the beneficial bronchodilation effect.

Front 16

___________ is the antidote for muscarinic agonist poisoning.

Back 16

Atropine

Front 17

Anticholinergic overdose is characterized by which of the following signs and symptoms? (select all that apply)

a. Hyperthermia

b. Most mucus membranes

c. Mydriasis

d. Urinary retention

Back 17

a,c, d

Rationale: Anticholinergic overdose is characterized by hyperthermia, hot dry flushed skin, dry mouth mydriasis, delirium, tachycardia, paralytic ileus, urinary retention, myoclonic movements, seizures, coma, and respiratory arrest.

Front 18

__________ is the specific antidote for anticholinergic overdose.

Back 18

Physostigmine

Front 19

Mrs. Briggs, age 57, has a history of two myocardial infractions in the past 3yrs. She presents to the physicians office with symptoms of an overactive bladder. She requests an anticholinergic medication that she saw advertised on television. You would expect the physician to do which of the following?

a. Order the anticholinergic medication

b. Order blood work to rule out a UTI and order the medication.

c. Order a urinalysis to rule out a UTI. and order the medication.

d. Explain to the client that the medication is contraindicated because of her medical history.

Back 19

d

Rationale: Anticholinergic drugs are contraindicated for patients with BPH, myasthenia gravis, hyperthyroidism, narrow angle glaucoma, tachy dysrhythmias, myocardial infraction, heart failure, or conditions associated with esophageal reflux.

Front 20

Mr. Brady age 75 is experiencing extrapyramidal symptoms secondary to an antipsychotic drug. Which of the following drugs would you expect the physician to order to relieve these symptoms?

a. Beta blockers

b. Anticholinergics

c. ACE inhibitors

d. Physostigmine salicylate

Back 20

b

Rationale: Anticholinergic drugs are given preoperatively to prevent anesthesia associated complications such as bradycardia, excessive respiratory secretions and hypotension.

Front 21

____________ is the drug of choice to treat bradycardia.

Back 21

Atropine

Front 22

Which of the following medications may be given to children because of its bronchodilation effects in the treatment of asthma and chronic bronchitis?

a. Ipratropium

b. Atropine

c. Hyoscyamine

d. Scopolamine

Back 22

a

Rationale: Ipratropium and tiotropium are anticholinergic medications given by inhalation for bronchodilation effects in the treatment of asthma and chronic bronchitis.

Front 23

Opthalmic anticholinergic preparations are indicated for _______________ and ____________ effects to aid in eye examination and surgery.

Back 23

mydriatic, cycloplegic

Front 24

Mr. Bates is diagnosed with IBS and the physician orders an antispasmodic. Which of the following drugs would you expect the physician to order?

a. Atropine

b. Hyoscyamine

c. Glycopyrrolate

d. Ipratropium

Back 24

c

Rationale: Anticholinergic drugs (ex. dicyclomine, glycopyrrolate) are indicated for antispasmodic effects in GI disorders. Historically they have also been used to treat peptic ulcer disease; however, they are weak inhibitors of gastric acid secretion and have been largely replaced other more effective medications (ex. proton pump inhibitors)

Front 25

You are asked to create a presentation for your anatomy and physiology class on cholinergic receptors. You explain that cholinergic (muscrinic) receptors are widespread throughout the body and are located in which of the following body parts? (select all that apply)

a. Mitochondria

b. Heart

c. Eyes

d. Glands

Back 25

b,c,d

Rationale: Cholinergic (muscarinic) receptors are widespread through the body producing effects in a variety of locations including the central nervous system, heart, smooth muscle , glands and eyes.

Front 26

Most anticholinergic drugs interact with muscarinic cholinergic receptors in the brain secretory glands, heart, and smooth muscle and are sometimes called _______________.

Back 26

antimuscarinic

Front 27

Anticholinergic drugs block the action of acetylcholine on which of the following systems?

a. Sympathetic nervous system

b. Parasympathetic nervous system

c. Musculoskeletal system

d. Genitourinary system

Back 27

b

Rationale: Anticholinergic drugs block the action of acetylcholine on the parasympathetic nervous system.

Front 28

Mr. Belcher is prescribed an anticholinergic drug by his physician. He likes to hike with his grandchildren. As his home care nurse you realize that part of Mr. Belchers education plan should include heart stroke prevention, because anticholinergic medications have which of the following effects?

a. increasing sweating and the risk for heart stroke and dehydration.

b. Causing postural hypotension and increased risk for falls and from exposure to the elements.

c. Causing bradycardia in older adults, which increases the risk for falls and from exposure to the elements.

d. Preventing sweating and heat loss and increasing the risk of heat stroke.

Back 28

d

Rationale: Anticholinergic drugs are commonly used in home care with children and adults. The home care nurse may need to teach older patients or caregivers that the drugs prevent the sweating and heat loss and increase risks of heat stroke if precautions to avoid overheating are not taken.

Front 29

A client presents to your emergency department with evidence of bradydysrhythmias. Which of the following is the treatment of choice for bradydysrhythmias?

a. Atropine 0.5mg administered IV every 3 to 5 mins.

b. Atropine 1mg administered IV every 3 to 5 minutes.

c. Atropine 0.25mg administered IV every 3 to 5 mins

d. Atropine 4mg administered IV every 3 to 5 mins.

Back 29

a

Rationale: Atropine is an important drug in the emergency drug box. According to ACLS guidelines atropine is the first drug to be administered in the emergency treatment of bradysrhythmias. Atropine 0.5mg should be administered IV every 3 to 5 mins and my be repeated up to 3mg (.03 to 0.04mg/kg)total dose

Front 30

Mr. Giancarlo age 80, who lives in a long term care facility is prescribed anticholinergic medications by his physician. Recently he has complained of blurred vision. You call the physician regarding these symptoms. You would expect to modify Mr. Giancarlo's care plan to include which of the following?

a. Falls prevention

b. Dietary modifications

c. Use of restraints

d. Occupational therapy

Back 30

a

Rationale: Older adults are especially likely to have significant adverse reactions because of slowed drug metabolism and the frequent presence of several disease processes. A patient who complains of blurred vision may need help with ambulation, especially with stairs or in other potentially hazardous environments. Obstacles and hazards should be removed if possible.

Front 31

Mrs. Beach age 45 is diagnosed with overactive bladder, asthmatic bronchitis and narrow angle glaucoma. She asks the physician to prescribe the same anticholinergic medication that her friend uses for her overactive bladder. Which of the following would you expect the physician to do?

a. Order the medication

b. Order the medication with scheduled routine blood work.

c. Decline the prescription preference because of the diagnosis of asthmatic bronchitis.

d. Decline the prescription because of the diagnosis of narrow angle glaucoma.

Back 31

d

Rationale: Normally, anticholinergics do not change intraocular pressure, but with narrow angle glaucoma they may increase intraocular pressure and precipitate an episode of acute glaucoma.

Front 32

Mr. Wright is diagnosed with irritable bowel syndrome. The physician orders anticholinergic medication. What is the reason for this decision?

a. To reduce the inflammation to the intestines.

b. To increase the frequency of the bowel.

c. To reduce the requency of bowel movements

d. To prevent a gastrointestinal bleed.

Back 32

c

Rationale: Anticholinergics may be helpful in reducing the frequency of bowel movements and abdominal discomfort associated with irritable colon or colitis.

Front 33

Mr. Devlin has been a paraplegic for 5yrs. He complains of increased incontinence, and the physician order anticholinergic medications. what is the reason for this decision?

a. To increase bladder capacity

b. to strengthen the detrusor muscles

c. To decrease bladder capacity

d. To decrease irritation to the wall of the bladder.

Back 33

a

Rationale: In infections such as cystitis, urethritis, and prostatitis, anticholinergic drugs decrease the frequency and pain of urination. The drugs are also given to increase bladder capacity in enuresis, paraplegia, or neurogenic bladder.

Front 34

Mr. Levitz is diagnosed with Parkinson's disease. The physician orders anticholinergic drugs. What is the reason for this decision?

a. To improve his gait

b. To decrease spasticity

c. To prevent fractures

d. To improve swallowing

Back 34

b

Rationale: Anticholinergic drugs are given for their central effects in decreasing salivation, spasticity, and tremors. They are used mainly in patients who has minimal symptoms, who do not respond to levodopa, or who cannot tolerate levodopa because of adverse reactions or contraindications. An additional use of anticholinergic drugs is to relieve Parkinson's like symptoms that occur with older anti-psychotic drugs.

Front 35

True or false?

Tertiary amines are excreted in the urine.

Back 35

True

Front 36

True or false?

Tertiary amines are uncharged lipid soluble molecules and therefor can cross the cell membranes readily.

Back 36

True

Front 37

True or false

Some belladonna derivatives and synthetic anticholinergics are quaternary amines. These drugs carry a positive charge and are lipid insoluble. Consequently, they do not cross the cell membrane.

Back 37

True

Front 38

________ is the prototype of anticholinergic drugs and is a naturally occurring belladonna alkaloid that can be extracted from the belladonna plant. It is well absorbed form the GI tract and rapidly excreted in the urine. It has a short duration except when used for ocular effects and it may last for several days.

Back 38

Atropine

Front 39

What are the Belladonna alkaloids and derivatives?

Back 39

1. Atropine
2. Opthalmic atropine
3. Homatropine
4. Hyoscyamine
5. Hyoscyamine
6. Ipratropium
7. Scopolamine
8. Tiotropium bromide

Front 40

These Belladonna's are used for Mydriatic cycloplegia, inflammation of uveal tract.

Back 40

1. Ophthalmic atropine
2. Homatropine
3. Scopolamine

Front 41

This Belladonna is used for antispasmodic antisecretory for GI and GU disorders.

Back 41

1. Hyoscyamine

Front 42

These Belladonna's are used for bronchodilation.

Back 42

1. Ipratropium
2. Tiotropium Bromide

Front 43

This belladonna is used for systemic use, antimetic, mydriatic, cycloplegia, inflamation of uveal tract.

Back 43

1. Scopolamine

Front 44

What are the antisecretory antispasmodic anticholinergics for GI disorders?

Back 44

1. Dicyclomine Hydrochloride
2. Glycopyrrolate

Front 45

What are the anticholinergics used in Parkinson's disease?

Back 45

1. Benztropine
2. Trihexyphenidyl

Front 46

What are the drugs used in urinary antispasmodics (overactive bladder)?

Back 46

1. Darifenacin hydrobromide
2. Flavoxate
3. Oxybutynin
4. Solifenacin succinate
5. Tolterodine
6. Trospium chloride

Front 47

_________ is a mixture of alkaloids in an aqueous alcohol solution. It is most often used for GI disorders because of its antispasmodic effect.

Back 47

Belladonna Tincture

Front 48

_________ is a semisynthetic derivative of atropine used as eye drops to produce mydrasis and cycloplegia. May be preferred because ocular effects do not last as long.

Back 48

Homatropine hydrobromide

Front 49

__________ is an anticholinergic drug chemically related to atropine. Used in nasal spray, it is useful in treating rhinorrhea due to allergies or the common cold. When used to treat COPD it acts as a bronchodilator.

Back 49

Ipratropium

Front 50

_________ depresses the CNS and causes amnesia, drowsiness, euphoria, relaxation, and sleep. Also, it is used in motion sickness.

Back 50

Scopolamine

Front 51

_________ is a dry powder in capsule from intended for oral inhalation with the handihaler inhalation device. Is indicated for daily maintenance treatment of bronchospasm associated with COPD.

Back 51

Tiotropium Bromide (spiriva)

Front 52

__________ and ________________ are older medications used to treat peptic ulcer disease. However, one is useful as an antispasmodic agent for treatment of IBS.

Back 52

Dicyclomine and glycopyrrolate.

Front 53

________ is used in the treatment of parkinsonism and extrpyramidal reactions caused by some antipyschotic drugs. This drug is contraindicated in glaucoma.

Back 53

Trihexyphenidyl

Front 54

____________ is a synthetic drug with both anticholinergic and anithistaminic effects. A major clinical use is to treat acute dystonic reactions caused by antipyschotic drugs and to prevent their recurrence in patients receiving long term antipyschotic drug therapy. It may also be given in small doses to supplement other antiparkinson drugs.

Back 54

Benztropine

Front 55

_____________ is a competitive antimuscarinic anticholinergic agent with selective affinity for M3 receptors involved in contraction of the urinary bladder. It is 98% protein bound and extensively metabolized in the liver by CYP3A4 and CYP2D6 enzymes. In some Caucasians and 2% African Americans are poor metabolizers of the drug and my require reduced dosages to avoid adverse effects.

Back 55

Darifenacin

Front 56

__________ was developed specifically to counteract spasm in smooth muscle tissue of the urinary tract. This drug relieves dysuria, urgency, frequency, and pain with genitourinary infections such as cystitis and prostatitis.

Back 56

Flavoxate

Front 57

____________ has direct antispasmodic effects on smooth muscle and anticholinergic effects. it increases bladder capacity and decreases frequency of voiding in patients with neurogenic bladder.

Back 57

Oxybutynin

Front 58

__________ is indicated for the treatment of overactive bladder with symptoms of urgency, urge incontinence, and frequency. Dosages should be reduced in individuals with moderate renal or liver impairment. This drug may prolong QT intervals especially at higher doses potentially resulting in dysrhythmias.

Back 58

Solifenacin

Front 59

_______________ inhibits bladder contraction decreases detrusor muscle pressure and delays the urge to void. It is more selective for muscarinic receptors in the urinary bladder than in other areas of the body. Reduced doses (1mg) are recommended for patients with hepatic dysfunction.

Back 59

Tolterodine

Front 60

____________ is an antimuscarinic anticholinergic drug for treatment of urgency, urge incontinence, and urinary frequency. This drug reduces the tone of smooth muscle in the bladder, exerting an antispasmodic effect. Because of its quaternary structure less than 10% of an orally administered dose is absorbed, and food further delays absorption. Must be taken on an empty stomach or 1hr before meals. It is eliminated by a combination of glomerular filtration and active tubular secretion. Beware of interactions with digoxin, procainamide, pancuronium, morphine, vancomycin, metformin, and tenofovir. These could lead to an increased serum concentration. Reduced dosages are recommended for patients with renal insufficiency and those older than 75yrs.

Back 60

Trospium

Front 61

What disorders are anticholinergic drugs contraindicated?

Back 61

Glaucoma, prostatic hypertrophy, reflux esophagitis, myasthenia gravis, and hyperthyroidism.

Front 62

What are the characteristics of a anticholinergic overdose?

Back 62

Hyperthermia, hot dry flushed skin, dry mouth, mydriasis (dilated pupils) delirium, tachycardia, paralytic ileus, urinary retention; myoclonic movements (sudden, brief, jerky, shock-like, involuntary movements) seizures, coma, and respiratory arrest.

Front 63

What is the antidote for an anticholinergic overdose?

Back 63

Physostigmine

Front 64

What is the antidote for for a muscarinic agonist poisoning?

Back 64

Atropine