pharm exam 1 CNS stimulants & adrenergic blocking drugs

CNS stimulants (adrenergic agonists) for ADHD

amphetamines

ADHD effects

altered norepinpehrine and dopamine neurotransmission in brain regions associated with attention, impulsivity and activity

symptoms: inattention, hyperactivity, impulsiveness

CNS stiumlant effects

stimulate release of norepinephrine and dopamine from CNS and peripheral nerves and block removal or norepinephrine and dopamine from the synapse

CNS stiumlant effects - CNS stimulation

increased focus, attention, alertness, mood, motor activity, talking

decreased appetite, weight, sleep, pain

CNS stiumlant effects - cardiovascular

increased HR, conduction and BP

CNS stiumlant effects - dependence

withdraw symptoms if abused

CNS stiumlant effects - abuse

stimulate reward centers in the brain t cause euphoria (schedule II controlled substances)

amphetamines for ADHD

CNS active (D) and less active (L) isomers

preffered admin 1x a day in morning after breakfast

amphetamines short duration

4 hrs

2-3x a day

adderall

amphetamines long duration

10 hrs

once a day

adderall XR

amphetamines side effects

weight loss

insomnia

cardiovascular stimulation

methylphenidate

commonly used to treat ADHD

same effects as amphetamines

methylphenidate short duration

4 hrs

2-3 x per day

ritalin

preferred once a day in the morning after breakfast

methylphenidate intermediate duration

8 hrs

1x a day

ritalin SR

methylphenidate long duration

12 hrs 1x a day
ritalin LA

adrenergic blocking drugs (adrenergic antagonists)

these drugs block responses caused by adrenergic nerve stimulation

adrenergic receptor blocking drugs

bind to adrenergic receptors but do not stimulate the receptor to cause a response

adrenergic neuron blocking drugs

inhibit the activity of adrenergic nerves

alpha 1 antagonist unselective drugs

labetalol

carvedilol

phentolamine

phenoxybenzamie

alpha 1 antagonist selective drugs

tamsulosin

doxazosin

alpha 2 antagonist unselective drugs

phentolamine

phenoxybenzamie

alpha 2 antagonist selective drugs

yohimbine

beta 1 antagonist unselective drugs

labetalol

carevdilol

propranolol

timolol

beta 1 antagonist selective drugs

metoprolol

atenolol

beta 2 antagonist unselective drugs

labetalol

carvedilol

propranolol

timolol

eye responses to alpha 1 receptor blocker

miosis

respiratory system responses to beta 2 receptor blocker

constriction

heart responses to beta 1 receptor blocker

decreaed force of contraction

decreased rate

decreased automaticity

decreased impulse conduction

arteries and veins responses to a1 and a2 receptor blocker

dilation

arteries and veins responses to b2 receptor blocker

constriction

GI responses to a1 receptor blocker

increased motility (b2 also)

relaxed sphincters

increased activity overall

kidney response to b1 receptor blocker

decreased renin release, angiotension II

urinary bladder response to B2 receptor blocker

detrousor constricted

urinary bladder response to a1 receptor blocker

sphincter relaxed

male reproductive organs response to a1 receptor blocker

impaired ejaculation

clinical use of alpha blocker

hypertension

benign prostatic hyperplasia

impotence

hypertension and a blockers

doxazosin

block a1 receptors from being activated by norepinephrine released from sympathetic nerves in blood vessles

blocks vasoconstriction to lower BP

benign prostatic hyperplasia and a blockers

enlarged prostate squeeze urethra and make it harder to urinate

tamsulosin blocks a1 stimulation and causes smooth muscle to relax, less pressure on urethra and urine flows more easily

impotence and a blockers

yohimbine used to increase penile blood flow to treat ED by blocking alpha 2 receptors

relax blood vessles and smooth msucle so more blood can flow to penis

yohimbine negative effects

can cause insomnia, anxiety, palpitations, tachycardia, chest pain, blurred vision, heart attack, seizures

adverse effects of alpha blockers - cardiovascular

reflex tachycardia

orthostatic hypotension (dizziness and fainting)

nasal congestion

adverse effects of alpha blockers - kidney

sodium retention; use care with edema

adverse effects of alpha blockers - CNS

dizzieness, drowsiness, anxiety

clinical use of B blockers

hypertension

angina pectoris

arrhythmias

chronic heart failure

migrain

glaucoma

hypertension and B blockers

metoprolol and atenolol

decrease cardiac output and decrease renin-angiotension (potent vasoconstrictor) by blocking B1 receptors

angina pectoris and B blockers

angina pectoris is chest pain/pressure/discomfort associated with myocardial ischemia

metoprolol goal is to decrease cardiac work to decrease need for O2 so less ischemia by blocking b1 receptors

arrhythmias and B blockers

metoprolol can reduce excessive activation of cardiac by blocking beta 1 receptors

chronic congestive heart failure and B blockers

carvedilol used to reduce excessive sympathetic stimulation

migraine headache and B blockers

propanolol used to prevent migraines by blocking beta receptors and stabilizing blood vessel and nerve activity involved in migrain development

glaucoma and B blockers

glaucoma is elevated intraocular pressure due to excessive fluid in the eye

timolol reduce aqueous humor formation

adverse effects of B blockers - CNS

lethargy, depression, fatigue, altered sleep

adverse effects of B blockers - respiratory

wheezing and bronchoconstriction in asthma and COPD

adverse effects of B blockers - cardiac

bradycardia, AV node block

adverse effects of B blockers - withdrawal

angina, hypertension, arrhythmias

adverse effects of B blockers - metabolic

excessive hypoglycemia and mask hypoglycemia symptoms in diabetes

adrenergic neuron blocking drugs

these drugs are agonists at receptros in teh CNS but this action blocks (inhibits) adrenergic nerve activity

inhibitors of sympathetic nerve outflow - centrally acting a2 adrenoceptor agonists

clonidine

clonidine mechanism of action

stimulate a2 adrenergic receptors on inhibitory nerves in the brainstem

decrease and block sympathetic nerve outflow to the heart and blood vessels

decrease blood pressure and heart rate

uses of adrenergic neuron blocking drugs

secondary to treat hypertension

opiod and nictoine withdrawal symptoms for severe pain

adverse effects of adrenergic neuron blocking drugs

drowsiness, fatigue, postural hypotension, impaired ejaculation, withdrawal rebound hypertension, dry mouth