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Pharmacology > Drugs Affecting the Autonomic Nervous System > Flashcards

Drugs Affecting the Autonomic Nervous System Flashcards

1
Q

Drugs affecting the autonomic nervous system

A 
Alpha2 Agonists
Alpha1 Antagonists
Beta Adrenergic Antagonists
Combined Alpha and Beta Adrenergic Antagonists
Muscarinic Agonists
Cholinesterase Inhibitors
Cholinergic Blockers
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2
Q

Alpha2 Agonists

A

Clonidine
Guanabenz
Guanfacine
Methyldopa

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3
Q

Alpha1 Antagonists

A 
Alfuzosin
Doxazosin
Prazosin
Silodosin
Tamsulosin
Terazosin
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4
Q

Beta Adrenergic Antagonists

A 
Acebutolol
Atenolol
Metoprolol
Nadolol
Nebivolol
Pindolol
Propranolol
Timolol
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5
Q

Combined Alpha and Beta Adrenergic Antagonists

A

Carvedilol
Labetalol
Epinephrine

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6
Q

Muscarinic Agonists

A

bethanechol (Urecholine)

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7
Q

Cholinesterase Inhibitors

A 
Donepezil
Galantamine
Memantine
Neostigmine
Pyridostigmine
Rivastigmine
Tacrine
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8
Q

Cholinergic Blockers

A 
Atropine
Benztropine
Darifenacin
Fesoterodine
Dicyclomine
Oxybutynin
Propantheline
Scopalamine
Solifenacin
Mirabegron
Tolterodine (Detrol)
Trihexyphenidyl
Trospium (Sanctura)
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9
Q

Clonidine Pharmacokinetics

A

Onset: Oral 30-60 minutes
Transdermal 2-3 days
Peak: Oral 3-5 hours
Duration: Oral 8 hours
Transdermal: 7 days (8 hours of effect after
patch is removed)
Half-Life: 12-16 hours. Up to 41 hours in impaired renal
function
Elimination: 40-60% unchanged in urine; 50%
metabolized in liver

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10
Q

Gunabenz Pharmacokinetics

A 
Onset: 60 minutes
Peak: 2-5 hours
Duration: 12 hours
Half-LIfe: 6 hours, prolonged in renal impairment
Elimination: <1% unchanged in urine
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11
Q

Guanfacine Pharmacokinetics

A

Onset: 1 hour
Peak: 1-4 hours
Duration: 24 hours
Half-Life: Adults - 17 hours, Younger Adults- 13 to 14 hr
Elimination: 50% unchanged in urine, 70% in urine
unchanged or as metabolites

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12
Q

Methyldopa Pharmacokinetics

A

Onset: 2-3 hours
Peak: 2-6 hours
Duration: 12-24 hours
Half-Life: 1.8 hour. Blood pressure reduction is
pronounced and prolonged in renal failure
Elimination: Extensively metabolized in liver; 70% in urine
as metabolites

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13
Q

Clonidine Interactions

A

-Alcohol, antihistamines, phenothiazines, barbiturates, benzodiazepines
Effect: additive sedation
Implications: Avoid concurrent use
-Beta Adrenergic Blockers
Effect: Attenuation or reversal of antihypertensive
effect of clonidine; may result in life-threatening
hypertension
Implications: Avoid concurrent use; if patient is
taking both drugs and withdrawal is required,
withdraw beta-adrenergic blocker first to prevent
excessive unopposed alpha stimulation that may
lead to malignant HTN.
-Nitrates, other antihypertensives
Effect: additive hypotensive effects
Implications: Avoid concurrent use
-Prazosin
Effect: Decreased antihypertensive effect of
clonidine
Implications: Choose alternative drug
-TCA’s
Effect: Block antihypertensive effects of clonidine
and may result in life-threatening HTN
Implications: Choose alternative antidepressant
-Verapamil
Effect: Synergistic pharmacological and toxic effects
may result in AV block and severe hypotension
Implications: Choose alternative calcium channel
blocker or antihypertensive

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14
Q

Guanabenz/Guanfacine Interactions

A

-Alcohol, antihistamines, phenothiazines, barbiturates, benzodiazepines
Effect: Additive sedative effects
Implications: Avoid concurrent use or choose
alternative antihypertensive
-Alcohol, nitrates, other antihypertensives
Effect: Additive hypotension
Implications: Avoid concurrent use or monitor
BP closely

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15
Q

Methyldopa Interactions

A

-Alcohol, antihistamines
Effect: Additive sedation
Implications: Avoid concurrent use
-Beta-adrenergic Blockers
Effect: May result in life-threatening HTN
Implications: Less likely with beta1 selective agents
same implications as clonidine
-Haloperidol
Effect: Potentiate antipsychotic effects or may
produce psychosis
Implications: Choose different antipsychotic
-Levodopa
Effect: Potentiate antihypertensive effects of
methyldopa and central effects of levodopa in
Parkinson’s disease
Implications: Avoid concurrent use; choose
alternative antihypertensive
-Lithium
Effect: Increased risk for lithium toxicity
Implications: Choose alternative antihypertensive
-Monoamine oxidase inhibitors (MAOIs)
Effect: Metabolites of methyldopa stimulate release
of endogenous catecholamines that are usually
metabolized by MAOIs; result is excessive SNS
stimulation
Implications: Avoid concurrent use
-Nitrates, other antihypertensives
Effect: Additive hypotension
Implications: Avoid concurrent use
-Phenothiazines, sympathomimetics, barbiturates,
amphetamines
Effect: May result in serious HTN
Implications: Avoid concurrent use
-Tolbutamide
Effect: Tolbutamide metabolism may be impaired,
resulting in enhanced hypoglycemic effects
Implications: Choose alternative hypoglycemic
-TCA’s
Effect: Attenuation or reversal of antihypertensive
effect of methyldopa
Implications: Avoid concurrent use; choose
alternative drugs for depression or HTN
-Herbals: licorice; yohimbe, ginseng
Effect: May affect electrolyte levels. May decrease
efficacy of methyldopa
Implications: Monitor blood pressure and inform
patient

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16
Q

Clonidine Dosing

A

For Hypertension:

ORAL ADULTS
Initial Dose: 0.1 mg bid PO (older adults may need lower dose)

Increase in increments of 0.1 mg PO in weekly intervals

Maintenance Dose: 0.1-0.3 mg bid PO

Max Dose: 1.2 mg BID

TRANSDERMAL
Initial Dose: Catapres 0.1 mg

After 1-2 weeks, if desired BP is not achieved, increase in increments of 0.1 mg/week

Comes in 0.2 mg and 0.3 mg patches

ORAL CHILDREN
12 years and older

Initial Dose: 0.1 mg bid

Increase in 0.1 mg increments at weekly intervals

Maintenance Dose: 0.1-0.3 mg bid

Max Dose: 2.4 mg/day

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17
Q

Clorpress Dosing

Clonidine HCl and Clorthalidone

A

For Hypertension:

Initial Dose: 0.1 mg clonidine plus 15 mg chlorthalidone once or twice daily

Max Dose: 0.6 mg clonidine plus 30 mg chlorthalidone

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18
Q

Guanabenz Dosing

A

For Hypertension:

Initial Dose: 4 mg bid

Increase in increments of 4-8 mg/day every 1-2 weeks until target BP achieved.

Max Dose: 32 mg bid

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19
Q

Guanfacine Dosing

A

For Hypertension:

Initial Dose: 1 mg daily at bedtime

May increase to 2 mg qd after 3-4 weeks if target BP not achieved; 2 mg dose may be given as 1 mg bid

Max Dose: 3 mg qd

20
Q

Methyldopa Dosing

A

For Hypertension:

ADULTS
Initial Dose: 250 mg bid or bid for first 48 ours

Increase in increments of 250 mg every 2 days until target BP is achieved: to minimize sedation, increase dose in evening. Smaller doses should be used in renal impairment

Maintenance Dose: 500-2,000 mg/day in 2-4 divided doses

CHILDREN
Initial Dose: 10 mg/kg/day in 2-4 divided doses

Max Dose: 65 mg/kg or 3,000 mg, whichever is less

21
Q

Alfuzosin Pharmacokinetics

A 
Onset: Unknown
Peak: 8 hours
Duration: Unknown
Half-Life: 10 hours
Elimination: 69% in feces; 24% in urine
22
Q

Doxazosin Pharmacokinetics

A 
Onset: 60-120 minutes
Peak: 2-3 hours
Duration: 24 hours
Half-Life: 22 hours
Elimination: 63% in bile/feces; 9% in urine
23
Q

Prazosin Pharmacokinetics

A 
Onset: 120-130 minutes
Peak: 1-3 hours
Duration: 6-12 hours
Half-Life: 2-3 hours
Elimination: 90% in bile/feces; 10% in urine
24
Q

Silodosin Pharmacokinetics

A 
Onset: unknown
Peak: 2.6 hours
Duration: Unknown
Half-Life: 13.8 hours
Elimination: 35.5% in urine; 55% in feces
25
Q

Tamsulosin Pharmacokinetics

A 
Onset: Unknown
Peak: 5 days
Duration: Unknown
Half-Life: 9-15 hours
Elimination: <10% unchanged in urine
26
Q

Terazosin Pharmacokinetics

A 
Onset: 15 minutes
Peak: 1-2 hours
Duration: 12-24 hours
Half-Life: 9-12 hours
Elimination: 60% in bile/feces; 40% in urine
27
Q

Doxazosin Dosing

A

For Hypertension:

Initial Dose: 1 mg daily at bedtime

Maintenance Dose: 2-16 mg daily. Depending on standing BP, increase dose in 2 mg increments until target BP is achieved. Doses >4 mg increase risk of postural hypotension.

For BPH:

Initial Dose: 1 mg daily at bedtime. Extended release form is 4 mg taken once daily at breakfast.

Maintenance Dose: 1-8 mg daily. Depending on the urodynamics and BPH symptoms, the dose is increased to 2 mg and then to 4 mg and 8 mg/daily. The recommended maximum dose is 8 mg. The titration interval is 1-2 weeks.

28
Q

Prazosin Dosing

A

For Hypertension:

Initial Dose: 1-2 mg bid or bid; take first dose at bedtime.

Maintenance Dose: 6-15 mg/daily in 2-3 divided doses. Depending on standing BP, increase dose in 1 mg increments with the larger dose being given at bedtime until target BP is achieved. Doses >20 mg/day usually do not increase efficacy.

29
Q

Silodosin Dosing

A

For BPH:

Initial Dose: 8 mg once daily with a meal

Starting dose may be 4 mg with increases to 8 mg as tolerated.

30
Q

Tamsulosin Dosing

A

For BPH:

Initial Dose: 0.1 mg daily 30 minutes prior to the same meal

May be increased after 2-4 weeks to 0.8 mg daily

31
Q

Terazosin Dosing

A

For Hypertension:

Initial Dose: 1 mg daily at bedtime

Maintenance Dose: 1-5 mg daily. Depending on standing BP, increase dose in 1 mg increments until target BP is achieved. Doses >20 mg/daily do not increase efficacy.

For BPH:

Initial Dose: 1 mg daily at bedtime

Increased in a stepwise fashion to 2, 5, and then 10 mg. Doses at 10 mg are usually required for clinical effect. Dose may be 10-20 mg daily. Four to 6 weeks are required to assess for beneficial response, so this is the interval for dosage adjustment.

32
Q

Alfuzosin Dosing

A

For BPH:

Initial Dose: 10 mg daily after the same meal

Maintenance Dose: 10 mg daily after the same meal

33
Q

Alfuzosin Interactions

A

-Ketoanazole, itraconazole, ritoniver
Effect: decrease metabolism and increase effects
of alfuzosin
Implication: Avoid concurrent use
-cimetidine, atenolol, diltiazem
Effect: increase level of alfuzosin and may increase
effects of atenolol and diltiazem
Implication: Monitor BP and HR
-Antihypertensives, calcium channel blockers, nitrates, and alcohol
Effect: Increased hypotension risk
Implication: Monitor BP or avoid concurrent use

34
Q

Prazosin Interactions

A

-Beta-adrenergic blockers
Effect: May enhance acute postural hypotension
following first dose of alpha1 adrenergic blocker
Implication: Select different alpha1 adrenergic
blocker. No adverse reaction seen with doxazosin or
terazosin.
-Clonidine
Effect: May decrease antihypertensive effect of
clonidine.
Implication: Avoid concurrent use
-Indomethacin
Effect: Antihypertensive action of prazosin may be
decreased.
Implication: Select different alpha1 adrenergic
blocker or different NSAID. No adverse reaction with
doxazosin or other NSAIDs.

35
Q

Silodosin Interactions

A

-Calcium channel blockers and thiazides
Effect: Increased incidence of dizziness and
orthostatic hypotension
Implication: Exercise caution and monitor for
adverse effects
-Azole antifungals, clarithromycin, and other strong CYP3A4 inhibitors
Effect: Ketoconazole increased Cmax and AUC
Implication: Concomitant use with strong CYP3A4
inhibitors contraindicated
-Diltiazem, erythromycin, verapamil, and other moderate CYP3A4 inhibitors
Effect: May increase plasma levels
Implication: Exercise caution and monitor for
adverse effects
-Phosphodiesterase type 5 inhibitors (e.g., sildenafil, tadalafil
Effect: Increased incidence of orthostatic
hypotension
Implication: Exercise caution and monitor for
adverse effects

36
Q

Tamsulosin Interactions

A

-Cimetidine
Effect: May increase blood levels of tamsulosin,
with increased risk for hypotension and toxicity
Implication: Select different histamine2 blocker if
one must be used

37
Q

Terazosin Interactions

A

-NSAIDs, sympathomimetics, estrogens
Effect: May decrease antihypertensive effects of
terazosin
Implication: Avoid concurrent use or select
doxazosin or another drug class for
antihypertensive therapy
-Verapamil
Effect: Increases serum terazosin levels and may
increase sensitivity to terazosin-vnduced postural
hypotension
Implication: Avoid concurrent use
-Finasteride
Effect: Increase in peak plasma concentration and
AUC of finasteride
Implication: Clinical significance unknown; monitor
for adverse effects of finasteride

38
Q

Doxazosin, prazosin, tamsulosin, terazosin, alfuzosin Interactions

A

-Alcohol, antihypertensives, nitrates
Effect: Additive hypotension
Implication: Avoid concurrent use or administer
first dose in the office and monitor BP closely

39
Q

Acebutolol Pharmacokinetics

A 
Onset: 60 minutes
Peak: 4-6 hours
Duration: 24-30 hours
Half-Life: 3-4 hours
Elimination: 30 to 40% in urine, 50 to 60% in feces/bile
40
Q

Atenolol Pharmacokinetics

A 
Onset: 60 minutes
Peak: 2-4 hours
Duration: 24 hours
Half-Life: 6-9 hours
Elimination: 50% unchanged in urine, rest in feces
41
Q

Metoprolol Pharmacokinetics

A 
Onset: 15 minutes
Peak: 90 minutes
Duration: 13-19 hours
Half-Life: 3-7 hours
Elimination: <5% unchanged in urine
42
Q

Nadolol Pharmacokinetics

A 
Onset: 5 days
Peak: 3-4 hours
Duration: 17-24 hours
Half-Life: 20-40 hours
Elimination: Unchanged in urine
43
Q

Nebivolol Pharmacokinetics

A

Onset: 15 minutes
Peak: 1.5-4 hours
Duration: Unknown
Half-Life: 12-19 hours based on genetic differences
Elimination: 38 to 67% in urine, 13 to 44% in feces

44
Q

Pindolol Pharmacokinetics

A 
Onset: 7 days
Peak: 1 hour
Duration: 24 hours
Half-Life: 3 to 4 hours
Elimination: 60 to 65% metabolites and 35 to 40% unchanged drug in urine
45
Q

Propranolol Pharmacokinetics

A 
Onset: 30 minutes
Peak: 60 to 90 minutes
Duration: 6-12 hours
Half-Life: 3-5 hours
Elimination: <1% unchanged in urine
46
Q

Timolol Pharmacokinetics

A 
Onset: Unknown
Peak: 1-3 hours
Duration: 12-24 hours
Half-Life: 4 hours
Elimination: Metabolites and unchanged drug in urine
47
Q

Beta Blockers Interactions

A

-Aluminum salts, barbiturates, calcium salts, cholestyramine, colestipol, NSAIDs, ampicillin, rifampin, salicylates
Effect: Decrease bioavailability and plasma levels
of beta adrenergic antagonists, possibly resulting
in decreased pharmacological effect
Implication: Avoid concurrent use. Separate
administration of cholestyramine or colestipol from
administration of beta blocker by 4 hour.
-Calcium Channel blockers
Effect: Potentiate effects of beta blockers
Implication: Do not administer within 24 hours of
each other. If must give both, monitor for heart failure
and decreased peripheral perfusion.
-Ciprofloxacin and other quinolone, cimetidine
Effect: Bioavailability of beta blocker metabolized by
CYP450 may be increased.
Implication: Select different antibiotic or different beta
blocker

Pharmacology (1 decks)

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