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199 Cards in this Set

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What are executive functions:

make higher level plans, balance checkbook, etc

5 drug classes to treat Parkinsons

Anticholinergics: block the cholinergic receptors (muscarinic receptors in the striatum)




Dopaminergics: convert to dopamine




Dopamine Agonists: stimulate the dopamine receptors




MAO-B inhibitors: inhibit the MAO-B enzyme which interferes with dopamine




COMT inhibitors: which inhibit the COMT enzyme that inactivates dopamine

Therapeutic goal of parkinson tx

give patient ability to carry out ADL

What is the Beer's Criteria

a list of drugs that should not be given to older adults.

1 type of drug given to Parkinson's patients on Beer's Criteria

Anticholinergic drugs.

Amantadine

Dopamine Releaser

Levodopa

Most effective drug for Parkinsons


Only works 2-5 years


75% of patients experience a 50% decrease in symptoms

2 types of loss of effect to Levodopa

1. Gradual loss


2. Abrupt loss

Solutions for treating gradual loss of effect to Levodopa.

COMPT inhibitor: Entacapone (Comtan)


Dopamine agonist: Pramaprexol

3 ways to manage side effects of Levodopa:

decrease dosage, giving amantadine in conjunction with Levodopa, or surgery called deep brain stimulation.

% of patients have movement disorder (dyskinesia) side effects from Levodopa

80%

What does an agonist drug do?

Stimulates the receptor & increases the response of the receptor.

2 types of receptors

-inhibitory


-excitatory

What will a dopamine agonist do?

Increase the action of Dopamine at the receptor.

Early stage treatment of Parkinson's

Pramipexole- Mirapex (a dopamine agonist)

Pharmacokinetics of Pramipexole-Mirapex

Pharmacokinetics, rapidly absorbed, can take with food.

Side effects of Pramipexole (Mirapex)

Nausea 28%


Dizziness 25%


Daytime somnolence 22%


Insomnia 17%


Constipation 14%


Weakness 14%


Hallucinations 9%

Side effects of Mirapex and Sinemet

Orthostatic hypotension 54%


Dyskinesia 47%


Hallucinations 17%

Adverse effects of levodopa

-nausea & vomiting


-dyskinesias (80% of patients)


-Cardiovascular effects: postural hypotension


-Psychosis: 20% of patients

Pharmacokinetics of Levodopa: where is it administered & where is it absorbed?

Administered orally & rapidly absorbed in intestine.

True or False: Food delays absorption by slowing gastric emptying.

True. And it competes with dietary proteins for blood brain transport.Nam

How much of each Levodopa drug reaches the brain?

2%

Name 2 inhibitory neurotransmitters used to treat Parkinson's

1. Dopamine


2. GABA

5 Classifications of Parkinson's

1. Dopamine Replacement


2. Dopamine Agonists


3. COMT Inhibitors


4. MAO-B Inhibitors


5. Dopamine Release

6 general parts to Pathophysiology of alzheimers

1. degenerative


2. vascular


3. infectious


4. metabolic


5. psychiatric


6. development of seniles plaques and neurofibrillary tangles.

Only cholinesterase inhibitor used for MILD, MODERATE, SEVERE

Donepezil (Aricept)

When to start taking Donepezil (Aricept)

As soon as symptoms start

Side effects of Memantine (Namenda)

Dizziness, H/A, confusion, constipation

What is difference between seizure and epilepsy

seizure is an isolated event, epilepsy is a disorder

Define automatism

follows complex partial seizure, repetitive, purposeless movements

Myoclonic Seizure

sudden muscle contraction that last for one second. (Like when your whole body jolts in bed)

Name a seizure that persists for 15-30 minutes or longer or a series of seizures during which the patient does not regain consciousness. This is a medical emergency.

Status epilepticus

2 seizure meds that suppress calcium influx

1. Valproic acid (review)


2. Ethosuximide (traditional)

4 traditional seizure meds that block NA influx into the cell

1. Phenytoin (traditional)


2. Carbamazepine (traditional)


3. Valproic acid (traditional)


4. Lamotrigine

1 medication that promotes potassium efflux: affect of repolarization

Ezogabine

What does an antagonist of Glutamate do?

Works against Glutamate

2 anti seizure drugs that antagonize glutamate

1. Felbamate


2. Topirimate

T or F is Dilantin is used to treat bipolar

False.

Define Nystagmus

Shaky eyeballs

Should you use an antipsychotic agent to treat an older adult?

NO!

Three types of schizophrenia symptoms

1. negative


2. positive


3. cognitive symptoms

Define labile affect of schizophrenia

one minute they are happy, the next they are hostile, the next they are neutral (all over the place.)

Define blunted affect of schizophrenia

no affect

First generation antipsychotics are classified by what?

Potency

Define Tardive Dyskinesia

uncontrolled, repetitive movement of the lounge in and out of the mouth.




Occurs late in treatment of schizophrenia with First generation Antipsychotics- cannot be reversed.

What is the most commonly prescribed class of antidepressant?

SSRI: Selective Serotonin Reuptake Inhibitors

What is the most widely prescribed SSRI in the US?

Fluoxetine, trade name Prozac

Define Bruxism

Grinding your teeth

What is serotonin syndrome?

adverse effect when patient is taking SSRI combined with MAOI: too much serotonin in the system. 2 to 72 hrs .

What is SNRI

Serotonin/Norepinephrine Reuptake Inhibitors

Important note about MAOI inhibitors

Don't take with other drugs.

Define Yawngasm

When you yawn and at the very end you have an orgasm. Side effect of TCA.

Acetylcholine is released by

1. all preganglionic neurons


2. parasympathetic postganglionic neurons




note: all motor neurons to skeletal muscles release acetylcholine. (NMJ)

Norepinephrine is released by

1. sympathetic postganglionic neurons

Epinephrine is released by

1. Adrenal medulla

3 cholinergic receptors

1. Nicotinic N


2. Nicotinic M


3. Muscarinic

5 adrenergic receptors

1. Alpha 1


2. Alpha 2


3. Beta 1


4. Beta 2


5. Dopamine (only responds dopamine)

Where are nicotinic n receptors found?

The cell bodies of all postganglionic neurons of parasympathetic & sympathetic systems.




-also found on cells of adrenal medulla.




remember: n for neurons

Where are nicotinic m receptors found?

located on skeletal muscle




remember: m for muscle.

Where are muscarinic receptors found?

all organs regulated by parasympathetic nervous system.

Where are adrenergic receptors found?


(alpha, beta, or both)

All organs (except sweat glands) regulated by the sympathetic nervous system.




note: adrenergic receptors are also found on organs regulated by epinephrine released from the adrenal medulla

What does activation of muscarinic receptors do to: Heart, lung, bladder, GI tract, sweat glands, sex organs, blood vessels, eye

Heart- decrease BP and HR


Lung- contract bronchi sm. muscles


Bladder-relax trigone & sphincter-release urine


GI-increases salivation,secretions, tone & motility


Sweat glands-general sweating


sex organs-erection (vasodilation)


blood vessels- vasodilation


eye- miosis (sm pupil) and focus for near vision

What does activation of nicotinic m receptors do?

contract skeletal muscle

Where are nicotinic m receptors located

NMJ- neuro muscular junction

What does activation of Nicotinic n receptors do?

Stimulate parasympathetic and sympathetic postganglionic nerves and release epinephrine from adrenal medulla.

Where are Nicotinic n receptors locates

all autonomic nervous system ganglia & adrenal medulla

What receptors can epinephrine activate?

1. all alpha (alpha 1 and alpha 2)


2. all beta (beta 1 and beta 2)





What receptors can norepinephrine activate?

1. all alpha (alpha 1& alpha 2)


2. beta 1



what receptors can dopamine activate?

1. alpha 1


2. beta 1


3. dopamine

where are alpha 1 receptors located in peripheral system?

eye


arterioles of skin, viscera, mucous membrane


veins


sex organs, male


prostatic capsule


bladder

what does alpha 1 receptor activation do in peripheral system?

eye- increased pupil (mydriasis)


arterioles-skin/viscera/mucusmem- constriction


veins- constriction


sex organs- ejaculation


prostatic capsule- constrict


bladdar- contraction of trigone/sphincter

where are alpha 2 receptors located in peripheral system?

presynaptic nerve terminals*




*alpha2 receptors in CNS are post sympathetic

what does alpha2 receptor activation do in peripheral system?

causes inhibition of transmitter release




function: regulate transmitter release

where are beta 1 receptors located in peripheral system?

-heart


-kidney

what does beta 1 activation do in peripheral system?

THINK 1 Heart!




heart- increase HR, increased force of contraction, increased AV conduction velocity




Kidney- release of renin

where are beta 2 receptors located in peripheral system?

Think 2 LUNGS!




arterioles (heart, lung, skeletal muscle)


Bronchi- dilation


Uterus- relaxation


Liver- Glycogenolysis


Skeletal muscle- enhanced contraction, glycogenolysis





Where are dopamine receptors located in peripheral system?

Kidney

What does activation of dopamine receptors do in peripheral system?

Dilation of kidney vasculature.

Six categories of cholinergic drugs

1. Muscarinic agonist


2. Muscarinic antagonist


3. Ganglionic stimulating agents (@nicotinic n)


4. Ganglionic blocking agents (@nicotinic n)


5. Neuromuscular blocking agents(@nicotinic m)


6. Cholinesterase inhibitors (indirect)

What does a cholinesterase inhibitor do?

Prevents breakdown of acetylcholine by acetylcholinesterase. Increases action of all cholinergic receptors. (INDIRECT)

Prototype Muscarinic Agonist

Bethanechol (Urecholine)

Therapeutic uses for Bethanechol (Urecholine)

Urinary retention- receives urinary retention by activating muscarinic receptors of urniary tract

Adverse effects of Bethanechol (Urecholine)

CV: hypotension & bradycardia


GI/GU: excessive salivation, increased secretion of gastric acid, cramps & diarrhea


Respiratory: exacerbation of asthma

Patient teaching for Bethanechol (Urecholine)

GI: take 1 hour before or 2 hours after meals to reduce gastric upset.




-Have a bedpan/bathroom readily available, Bethanchol (Urecholine) acts rapidly on intestine and urinary tract.

Prototype Muscarinic Antagonist (Anticholinergic Drug)

Atropine

Therapeutic uses for Atropine

Pre anesthesia- decreases secretions


During eye surgery- increases pupils (myadraisis)


Reverse Muscarinic Agonist Toxicity


Increases HR


Decrease GI hypertonicity/hypermotility (dysentary)





Patient teaching for Atropine/ Anticholinergic Drug

Decreased salivation- sip water, chew sugar free gum, avoid sugar


Blurred vision- avoid hazards


Photophobia- wear sunglasses


Urinary retention- void prior to dosing


Constipation- increase fiber and fluid


No sweat- hyperthermia risk


Tachycardia- monitor pulse



Drug Drug interactions with Atropine

Antihistamines, tricyclic antidepressants, phenothiazines have antimuscarinic action and can cause excessive muscarinic blockade.

What does a reversible cholinesterase inhibitor do?

Binds reversibly to cholinesterase and prevents its degradation of acetylcholine, causing increase in available acetylcholine and enhancing cholinergic actions.

Prototype reversible cholinesterase inhibitor

Neostigmine (Bloxiverz, Prostigmin)

Neostigmine

Bloxiverz, Prostigmin

Bloxiverz, Prostigmin

Neostigmine- reversible cholinesterase inhibitor

Indications for Neostigmine (Bloxiverz, Prostigmin)

Tx of myasthenia graves

Adverse effects of Neostigmine (Bloxiverz, Prostigmin)

Toxic levels result in paralysis of respiratory muscles. Toxicity = SLUDGE and the Killer Bs

Cholinesterase Inhibitor Toxicity

SLUDGE and the Killer B's:


Salivation


Lacrimation


Urination


Diaphoresis/Diarrhea


Gastrointestinal cramping


Emesis


Bradycardia


Bronchospasm


Bronchorreah (excessive mucous)



Irreversible cholinesterase inhibitors

Highly toxic, insecticides, used in WWII as nerve agents- only clinical application: glaucoma to reduce intraocular pressure.

Neuromuscular Blocking Agent prototype

Succinylcholine (Anectine, Quelicin)

Succinylcholine (Anectine, Quelicin)

Neuromuscular Blocking Agent

Indication for Succinylcholine

muscle relaxation for surgery, mechanical ventilation, electroconvulsion therapy.

Contraindications for Succinylcholine (Anectine, Quelicin)

contraindicated for patient with low pseudocholinesterase activity, hx/fx of malignant hyperthermia, predisposition for hyperkalemia

Patient education with Succinylcholine (Anectine, Quelicin)

Succinylcholine (Anectine, Quelicin) can cause muscle pain, this is not unusual.

Four basic mechanisms of drug activation at adrenergic receptors.

1. Direct receptor binding


2. Promotion of NE release


3. Inhibition of NE reuptake


4. Inhibition of NE inactivation (inhibit monamine oxidase)

What happens when a drug inhibits monamine oxidase?

It inhibits NE inactivation and increases activation at adrenergic receptors.

2 major classes of adrenergic agonists

1. Catecholamines


2. Noncatecholamines

3 basic and important aspects of catecholamine class:

1. not available for PO


2. short duration of action


3. cannot cross BBB

3 basic and important aspects of noncatecholamine class:

1. available by PO


2. longer duration of action


3. can cross BBB

2 examples of noncatecholamines

1. Ephedrine (decongestant)


2. Phenylephedrine (nasal decongestant)

Therapeutic application of activation at alpha 1

vasoconstriction, hemostasis, nasal decongestions, elevation of blood pressure, mydriasis

Therapeutic application of activation at alpha 2

none!

Therapeutic application of activation at beta 1

heart failure, heart block, cardiac arrest, shock, av heart block

Therapeutic application of activation of Beta 2

asthma, preterm labor

Which are more selective, adrenergic agonists or adrenergic antagonists?

adrenergic antagonists.

2 major groups of adrenergic antagonists

1. alpha adrenergic blocking agents


2. beta adrenergic blocking agent

5 therapeutic applications for alpha blockade

1. HTN


2. revers toxicity from alpha 1 agonists


3. BPH


4. Pheochromocytoma


5. Raynaud's Disease

4 adverse effects of alpha blockade

1. orthostatic hypotension


2. reflex tachycardia


3. nasal congestion


4. inhibition of ejaculation

PRAZOSIN

prototype alpha blocker/ alpha adrenergic antagonist.

Indication for PRAZOSIN

only approved for HTN (but can be useful for BPH)

Adverse effects of PRAZOSIN

FIRST DOSE EFFECT: extreme orthostatic hypotension. Also reflex tachycardia and nasal congestion.

Therapeutic application of Beta Blockade (10)

-angina


-HTN


-cardiac dysrhthmias


-MI


-reduction of preoperative mortality


-heart failure


-hyperthyroidism


-stage fright


-migraine prophylaxis

Adverse effects of beta 1 blockade (4)

-bradycardia


-reduced CO


-precipitation of heart failure


-av heart block


-rebound cardiac excitation

adverse effects of beta 2 blockade (2)

-bronchoconstriction (contraindication in patients w/ asthma)


-hypoglycemia from glycogenolysis inhibition

2 adverse effects in neonates from beta 1 and beta 2 blockade

1. beta blockers can remain in circulation for several days


2. must be monitored for bradycardia, respiratory distress and hypoglycemia 3 to 5 days after birth

what is the indication for dopamine?

shock & heart failure (low does, renal perfusion only)

what is the indication for Dobutamine?

Heart failure only

what receptors does Dobutamine act on?

Beta 1 only

what receptors does Albuterol act on?

Beta 2 receptor specific

What class is albuterol?

noncatecholamine adrenergic agonist

what class is PROZOSIN?

alpha blocker- alpha adrenergic antagonist

what are the indication for PRAZOSIN

HTN, but can benefit men with BPH

what are the pharmakinetics of PRAZOSIN and TERAZOSIN. What is the main difference?

Both:


administered PO


hepatic metabolism


excretion in bile


TERAZOSIN:


prolonged half life, cannot take with food.

What should you advise to a patient taking an alpha blocker antagonist? (plus name 2 alpha blocker antagonists)

BEWARE FIRST DOSE EFFECT. (Prosazin, Terazosin)

-Zosin

Alpha Adrenergic Antagonist

-Amine

catecholamine, adrenergic agonist

-Prolol

beta blockers

First generation nonselective beta blocker

Propranolol

second generation selective beta blocker

Metoprolol

2 examples of centrally acting alpha 2 agonist

Clonidine & Methyldopa

indications for Clonidine

HTN, severe pain, ADHD

indications for methyldopa

HTN in pregnancy

contraindications for Methyldopa

active liver disease

advice for patients taking Clonidine

take at bedtime to avoid daytime sedation. advise against rapid discontinuation.

contraindications for Clonidine

adverse in pregnancy, can be abused.

Which class of drugs acting on adrenergic receptors? PO. highly lipid soluble, extensive first pass effect, widely distributed, undergoes hepatic metabolism and urinary excretion.

Beta blockers

3 cardinal symptoms of parkinson's disease

-bradykinesia (slow movement)


-postural instability


-rigidity


-tremors



how many new cases of parkinson's disease each year?

60,000 new cases / year

These patients frequently exhibit sx of dementia, depression, and impaired memory

Parkinson's patents

Parkinson's is a disorder of the _________system, a complex neuronal network that regulates movement.

extrapyramidal system

2 neurotransmitters that are off in Parkinson's disease

1. not enough dopamine


2. too much acetylcholine

What type of transmitter is Dopamine in the CNS?

Inhibitory

What type of transmitter is Acetylcholine in the CNS?

Excitatory.

What is the underlying cause of loss of dopamine in CNS in Parkinson's?

Loss of Dopamine neurons in substantial negra of brain.

What is the cause of Parkinson's?

Unknown: environmental and genetic factors

What other inhibitory neurotransmitter decreases along with dopamine in Parkinson's disease?

GABA

In a healthy _________, Dopamine is released from neurons in the __________ ________ and inhibits the firing of neurons that release _____________. Neurons located within the ________release ____________, excite the GABA, and controlled movement results.

Striatum


Substantia Nigra


GABA


Striatum


Acetylcholine

Safety risks to think about with Parkinson's patients as a nurse

-use bed alarms


-fall risk


-non skid shoes


-help with executive function

What is COMT inhibitor and what does it do

Inhibits Catacholomethyltransferase- keeps it from breaking down dopamine, epinephrine, norepinephrine.

What is an MAO-B inhibitor, what does it do?

It inhibits the MAO-B enzyme which interferes with dopamine. You will then have more dopamine on hand.

First group of drugs used to tx Parkinson's

Anticholinergic Agents.

Example of anticholinergic agent first used in Parkinson's disease tx.

Benztropin (Cogentin)

Side effect of anticholinergic agents

drowsiness, dizziness, headache, anorexia, dry mouth- on BEERS Criteria list.

Drugs used in dopamine replacement (undergoes conversion of dopamine in brain and activates receptors

Levodopa and Levodopa/Carbidopa

Mose effective drug for tx Parkinson's

Levodopa

How long will a patient be on Levodopa before it stops working?

2 to 5 years

2 types of loss associated with loss of effect to Levodopa

1. Gradual loss


2. abrupt loss

3 solutions to gradual loss of effect from Levodopa

-shorten dosing interval


-COMPT inhibitor like Entacapone (Comtan)


-give a direct dopamine agonist- Mirapex, Pramaprexol

this Parkinson's drug competes w/ dietary proteins to cross the BBB and thus can't be given with food, especially a high protein diet.

Levodopa

What fraction of Levodopa reaches the brain?

25

How is Levodopa administered and how is it absorbed? Where is it metabolized?

Orally. Absorbed rapidly in the liver. Metabolized in the periphery.

What class of drug is PRAMIPREXOLE?

Dopamine agonist

Pharmokinetics of Pramipexole

PO


Widely distributes


plasma levels peak 1-2 hours


drug eliminated unchanged in urine

Nursing assessments for PRAMIPEXOLE

-assess for hallucinations/confusion


-monitor BP and ECG


-assess for drowsiness and somnolence


-assess for signs of parkinson

Lab considerations for PRAMIPEXOLE

increase dosing interval if creatinine clearance is less than 60 mL per min

Side effects for PRAMIPEXOLE alone & w/ Levodopa

alone: nausea, dizzy, daytime somnolence, insomnia, constipation, weakness, hallucination, IMPULSE CONTROL disorder


w/ levodopa: orthostatic hypotension, dyskinesia

Lab considerations for Levodopa/Cardopa (Sinemet)

-may increase serum glucose


-monitor hepatic & renal function


-may cause anemia


-may cause high WBC

Drug interactions for Levodopa/Cardopa

-MAOI- hypertensive crisis


-first generation antipsychotics (block dopamine receptors)

This drug may darken sweat or urine

Levodopa

What class of drug is ENTACAPONE (Comtan)

COMPT inhibitor

What does ENTACAPONE (Comtan) tx?

Parkinson's

True or False- You can use ENTACAPONE (Comtan) alone to tx Parkinson's

False- it is only indicated for use with Levodopa/Carbidopa. It has no effect on its own.

These two drugs used to tx Parkinson's may not be used on their own- have no effect on their own

Carbidopa and Entacapone

How does ENTACAPONE work in the body?

It decreases metabolism of levodopa in peripheral tissues by inhibiting COMT. Increases half life of levodopa by 50 to 70%


This drug increases half life of Levodopa by 50 to 75%

ENTACAPONE (Comtan)

Nursing interventions for use of ENTACAPONE (Comtan) in Parkinson's tx

-assess Parkinson's sx


-monitor for neuroleptic malignant syndrome



What is neuroleptic malignant syndrome & what Parkinson's drug is it associated with?

-elevated temp


-muscular rigidity


-altered concouslness


-elevated CPK




-ENTACAPONE (Comtan)

This Parkinson's drug increases risk of hallucinations in geriatric patients

PRAMIPEXOLE (Mirapex)

% of patients on Levodopa that experience dyskinesias

80%

% of patients on Levodopa that experience psychosis

20%- visual hallucinations, vivid dreams , paranoia

What class of drug is SELEGILINE (Eldepryl, Zelapar) ? What is it used to treat?

MAO-B inhibitor used to tx Parkinson's

Can SELEGILINE (Eldepryl, Zelapar) be used alone or must it be used in combination with Levodopa?

SELEGILINE (Eldepryl, Zelapar) can be used alone or in combination with Levodopa.

How does SELEGILINE (Eldepryl, Zelapar) work in the body?

It causes selective, irreversible inhibition of MAO-B, the enzyme that normal deactivates dopamine in the striatum. It suppress the destruction of dopamine, thus prolonging the effects of levodopa.

What are the pharmakinetics of SELEGILINE (Eldepryl, Zelapar)

SELEGILINE (Eldepryl, Zelapar) is available as an oral tablet/capsule, undergoes rapid GI absorption, can cross BBB, undergoes hepatic metabolism and renal excretion.

2 metabolites of SELEGILINE (Eldepryl, Zelapar) that are CNS stimulants

-1 amphetamine


-1- methamphetamine

drug drug interactions with SELEGILINE (Eldepryl, Zelapar)

-concurrent use with meperidine or other opiod analgesics may result in fatal reaction- sweating, rigidity, hypotension, coma.


-SSRI- may cause serotonin syndrome


-tricyclic antidepressants-systole, diaphoresis, HTN, seizures


-may initially increase risk of side effects of levodopa/carbidopa


-drug + tyramine continent foods can causeHTN reaction

Education for patients on SELEGILINE (Eldepryl, Zelapar)- taking more than 20mg per day

avoid tyramine containing foods- alcoholic beverages, caffeine, OTC cold/cough meds.

What class of drug is Benztropine (Cogentin) & what does it treat?

Centrally acting anticholinergic drug tx Parkinson's

This is the oldest med used to tx Parkinson's, now second line.

Benztropine (Cogentin)

What does Benztropine (Cogent) do in the body?

Blocks muscarinic receptors in striatum which improves balance bt dopamine and Ach. Reduces tremor and rigidity but not bradykinesia

What cardinal sx of parkinson's can Benztropine (Cogent) relieve

-tremor


-rigidity

This parkinson's drug is on BEERS list for its CNS side effects of sedation and confusion for geriatric patients

Benztropine (Cogent)