In the heart, increases heart rate, force of contraction, and velocity of conduction in AV noce

In the Kidney, releases renin

muscarinic agonist

Used for urinary retention

Constricts bronchi and increased HR so dont use for patients with asthma, and hyperthyriod patients

muscarinic agonists

used in glaucoma: constricts pupils in eye which would decrease pressure

muscarinic antagonists (anticholinergic drugs)

Increases heart rate, decreases secretion from exocrine glands, relaxes bronchi, detrusor muscle and GI tract; causes mydriasis

Adverse Effects: dry mouth, blurred vision, increase intraocular pressure, urinary retention, constipation, anhidrosis, tachycardia, asthma

Neostigmine (Prostigmin)

"Reversible" Cholinesterase Inhibitors

Identical to muscarinic agonist response

Increases force of contraction in skeletal muscle, mild stimulation of the CNS

Used for Myasthenia gravis, used postoperatively to reverse muscle paralysis

Precaustions: Obstruction of GI Tract, Peptic ulcer disease, asthma, coronary insufficiency, hyperthyroidism

autoimmune disease; patient has periods of being ok then periods of fatigue

Treated with cholinesterase inhibitors

prevent acetylcholine from activating nicotinicM

cannot cross BBB

"Drug of choice for murder"

Ultrashort acting, muscle relaxation, no affect on the CNS

Adverse Effects: prolonged apnea in patients genetic tendency for slow acetylators, malignant hyperthermia,  postoperative muscle pain, hyperkalemia

Drug Interactions: antibiotics potentiate succinylcholine (aminoglyosides,, tetracyclines

Adrenergic agaonists

cannot be used orally, brief duration of action, cannot cross the BBB

Adrenergic Agonists

can be given orally, metabolized slowly by MAO (longer half life)

More able to cross BBB

Alpha 1 and alpha 2

Beta 1 and Beta 2

vasoconstriction, hemostasis, nasal decongestion, adjunct to local anesthesia, elevation of BP

Drugs: epinephrine, norepinephrine, phenylephrine, ephedrine, dopamine

Adverse effects: hypertension, necrosis, bradycardia,

works on cardiac arrest, heart failure (increases force of contraction), shock (increases HR), atrioventricular heart block (enhances conduction of AV node

adverse effects: altered HR or rhythm, angina pectoris (increases oxygen demand to heart by increasing HR and force of contraction)

for asthma but need to be specific, delay of preterm labor (relaaxes uterine smooth muscle

Adverse effects: hyperglycemia (promotes breakdown of glycogen into glucose), tremor (from activation of skeletal muscle)

severe allergic response

causes hypotension, bronchoconstriction, edema of glottis

Treat with epinephrine

adrenergic agonists

delay absorption of local anesthetic, control superficial bleeding, elevate BP, mydriasis during opthalmolocic procedures, overcome AV block, bronchial dilation in asthma, for anaphylactic shock

Adverse Effects: hypertensive crisis, dysrhythmias, angina, necrosis, hyperglycemia

Drug Interactions: MAO inhibitors, tricyclic antidepressants, alpha-adrenergic blocking agents, beta adrenergic blocking agents

Adrenergic agonist

Used for hypotensive states and cardiac arrest

does not activate beta 2 receptors

Does not promote hyperglycemia, cause necrosis with extravasation,

Drug interactions: MAOI, TCA, general anesthetics, adrenergic blocking agents

Adrenergic agonist

Receptor for beta 1 and beta 2

used for AV heart block and arrest,  used for bronchodilation in asthma (not used anymore), bronchospasm during anesthesia

Adverse effects: tachydysrhythmias, angina pectoris, hyperglycemia

drug interactions: MAOI, TCA, beta adrenergic blockers

Adrenergic agonists

used of shock (increases cardiac output and renal perfusion), heart failure (increases contractility)

Adverse effects: tachycardia, dysrhythmias, anginal pain, necrosis with extravasation

Drug Interactions: MAIO, TCA,

adrenergic agonists

Beta 2 receptor

used in asthma (selective for beta 2)

adverse effects: minimal therapeutic doses, tremor, and tachycardia

cause direct blockade of adrenergic receptors, with one exception all produce reversible (competitive) blockade, more selective than adrenergic agonists

Two Groups: 1) alpha adrenergic blacking agents 2) beta adrenergic blocking agents

Used in hypertension (lowers BP), benign prostatic hyperplasia, Raynauds disease, orthostatic hypotension,

Adverse effects: nasal congestion, inhibition of ejaculation, sodium retention and increased blood volume

Drugs: prazosin, terazosin, doxazosin, tamsulosin, alfuzosin (***ends in ZOSIN)

Beta Adrenergic Antagonists

(Beta blockade)

used in angina pectoris, hypertension cardiac dysrhythmias, MI, heart failure, hyperthyroidism, migraine, stage fright, glaucoma

Adverse effects of beta 1 blockade: bradycardia, reduced cardiac output, AV heart block,

Adverse effects of beta 2 blockade: bronchoconstriction, inhibition of glycogenolysis

beta adrenergic antagonists

blocks caardiac receptors (decreases cardiac output), non selective beta 1 and 2

used hypertension, angina, dysrhythmias, and MI

Adverse effects: bronchoconstriction, bradycardia, AV heart block, Heart failure, inhibition of glycogenolysis

Drug interactions: calcium channel blockers (diltiazem & verapamil) and insulin

Contraindictions: severe allergy, diabetes hypoglycemia, psychiatric disorders

Indirect acting antiadrenergic agent

decrease norepinephrine release

Indirect acting antiadrenergic agent

reduce impulses along the sympathetic nerves

Indirect acting antiadrenergic agent: adrenergic neuron blocking agent

Depletion of NE from postganglionic sympathetic neurons, can cause depletion of transmitters, slows heart rate, reduces caardiac output, used in sedation and severe depression

indirect acting antiadrenergic agents: centrally acting alpha 2 agonists

used for hypertension by decreasing BP and pain, use din minimal orthostatic hypotension

adverse effects: drowsiness, xerostomia, rebound hypertension,

indirect acting antiadrenergic agents

lowers BP (in supine and standing) by acting at sites within the CNS, causes alpha 2 activation, vasodilation,

used for hypertension (no longer first line drug)

adverse effects: positive coombs test and hemolytic anemia, hepatotoxicity, orthostatic hypotension

Neurodegenerative disorder of the extrapyramidal system associated with disruption of neurotransmission in the striatum

Imbalance between dopamine nad aCh

Characterized by: dyskinesias and akinesia

* most commonly used drugs for PD*

activate dopamine receptors

Ex: levodopa

used for PD

prevent activation of cholinergic receptors

EX: benztropine

dopaminergic agents

promotes dopamine synthesis

used in PD

rapid absorption of small intestine, good delays absorption, high protein foods reduce effect

Adverse effects: nausea and vomiting, dyskinesias, psychosis, darken sweat and uring, drug holidays

drug interactions: first generation antipsychotics, MAOI, anticholinergics, pyridoxine (Vit B6)

used for PD

no adverse effects, increases the available levodopa in CNS and allows decrease of levodopa dosage

effects come mainly from levodoopa when given in combo

levodopa/carbidopa= sinemet

Carbidopa alone is for investigational use

First line drugs for PD

direct activtion of dopamine receptors in striatum

compared to levodopa: less effective, dont compete with dietary proteins, lower incidence of response failure

Two types: 1) derivative of ergot (usually not used, nonselective) 2) nonergot derivates

 Example: pramipexole (mirapex)

used alone in early PDand with levodopa in advanced stages of PD

also use din restless leg syndrome

Adverse effects: monotherapy=nausea, vomiting, insominia, weakness, constipation, hallucinations; combined= orthostatic hypotension and dyskinesias, and increase in hallucinations

selective reversible inhibitor of COMT

only for use with levopoda

increases levodopa availability by inhibiting COMT, which decreases production of levodopa metabolites that compete with levodopa for transport

Adverse effects: from the increasing levodopa levels

second and third line of use for PD

combo with levodopa can reduce the wearing off effect

MAO-B inhibitors

Inhibits dopamine breakdown

suppresses destructionof dopamine derived from levodopa and prolong the effects of levodopa

adverse effects: insomia when used alone

used with mild to moderate alhezimers

prevent breakdown of ach, may help slow progression of disease

Only three recommended: donepezil (aricept), galatamine, rivastigmine (exelon)

first drugs in new class of NMDA areceptor antagonists

used for moderate to severe AD

Better tolerated than cholinesterase inhibitors

adverse effects: dizziness, headache, confusion, constipation and aviod use in patients with renal impairment

antiepileptic drug

selective inhibition of sodium channels

adverse effects: nystagmus, sedation, ataxia, diplopia, cognitive impairment, skin rash, birth defects

Drug interactions: decrease effects of oral contraceptives, warfarin, and glucocorticoids, increases levels of diazepam, isoniazid, cimetidine, alcohol, and valproic acid

Used for epilepsy, bipolar disorder, trigeminal and glossopharyngeal neuralgias

adverse effects: nystagmus, ataxia, leukopenia, anemia, thrombocytopenia birth defects, hypo-osmolarity, rash , photosensitivity NO GRAPEFRUIT JUICE

used for seizure disorders, bipolar disorder, migraine

adverse effects: gi effects, hepatotoxicity, pancreatitix, neural tube defects

used for epilepsy, promotes sleep and sedation

replaced by newer drugs

Involuntary contraction of muscle or muscle group

Causes: epilepsy, hypocalcemia, pain syndroms, and trama

relieve local muscle spasm, decrease local muscle paon, increase range of motion

one is not superior to the other

Adverse Effects: generalized CNS depression, hepatic toxicity, physical dependence

DOES NOT TREAT SPASTICITY

movement disorders of CNS origin

Most common causes: multiple sclerosis, and cerebral palsy

Characteristics: heightened muscle tone, spasm, loss of dexterity

Drugs: Baclofen, diazepam, dantrolene

acts in the CNS specifically the spinal cord, supresses hyperactive reflexes, many mimic the action of GABA on spinal neurons

Used for multiple sclerosis, spinal cord injury, cerebral palsy NOT WITH STROKE, supresses resistance to passive movement, no effect on skeletal muscle (used for spasticity)

Adverse effects: no antidote for overdose, gradual withdrawal, cns depressant, GI symptoms, urinary retention

Acts in CNS, member of the benzodiazepine family, the only one labeled to treat spasticity, mimics action of GABA

Adverse Effect: sedation

acts directly on skeletal muscle, not much on smooth muscle or cardiac, not in CNS

Used for spasticity associated with multiple sclerosis, cerebral palsy, spinal cord injury, BUT CAUSES REDUCTION IN STRENGTH, malignant hyperthermia

Adverse Effects: hepatic toxicity, muscle weakness, drowsiness, diarrhea