Exam #2

• Therapeutic: Drug to restore peristalsis or treat urinary retention
• Pharmacologic: Cholinergic agonist, muscarinic agonist (direct acting)

• Stimulated smooth muscle contraction. Restore smooth muscle tone and peristalisis following general anesthesia. Relaxes urinary sphincters and causes detrusor muscle of the bladder to contract (resulting in voiding)
• Off label: treatment of adynamic ilius and gastric atony

interacts indirectly with muscarinic receptors to cause body responses typical of parasympathetic stimulation. It is not destroyed by AchE; therefore, its actions are more prolonged than those of Ach.

• Route(s): PO, subcut
• Absorption: Poorly absorbed PO, well absorbed subcut
• Distribution: Widely distributed; does not cross the blood brain barrier
• Primary metabolism: Unknown
• Primary excretion: renal
• Onset of Action: PO: 30 min; subcut 5-15 min
• Duration of action: PO: 1-6 h; subcut: 2h

use with extreme caution in patients with disorders that could be aggravated by increased contractions of the GI tract, such as suspected bowel obstruction, recent GI surgery, an active ulcer, or an inflammatory disease urinary obstruction, recent bladder surgery, cystitis, asthma or COPD, MI, severe bradycardia, hypotension, hypertension, peritonitis, epilepsy, and parkinson's disease

• Concurrent use of AchE inhibitors should be avoided because it also stimulated muscarinic reseptors and excessive parasympathetic activity will result
• Concurrent use of ganglionic blockers may result in a rapid fall in BP
• Procainamide, quinidine, atropine, and epinephrine antagonize the effects of bethanechol
• Herbal/Food interactions: Unknown

Category C

Administration of atropine quickly reverse most symptoms (N&V, abd cramping, salivation, and hypotension)

• monitor BP and pulse, observe for adverse effects for at least one hour following subcut admin
• monitor for early signs of overdose, which include salivation, sweating, flushing, abd cramping, and nausea
• Observe and record pts response
• monitor resp status
• when ambulating, supervise the pt because of poss blurred vision

• Make position changes slowly to prevent dizziness and poss fainting
• Do not stand still for prolonged periods; sit or lie down at first indication of faintness
• Do not drive because of poss drowsiness or dizziness
• Do not breast-feed without approval of health care provider

• Carbachol (Isopto Carbachol, Miostat)
• Cevimeline (Evoxac)
• Pilocarpine (Isopto-Carpine, Ocusert, Salagen)

• Therapeutic: Agent for MG
• Pharmacologic: Indirect-acting cholinergic agonist, AchE inhibitor

• increases the strength of skeletal muscle contractions and delays fatigue
• increases peristalsis, bronchoconstriction, bradycardia, and hypotension
• relieving postoperative abd distension and urinary retension and in reversing the effects of nondepolarizing muscle relaxants

inhibits the action of AchE at cholinergic synapses, which allows Ach to accumulate and cause a greater effect.

• Route(s): PO, IM, IV, and subcut
• Absorbtion: PO: only 1-2% is absorbed. The oral dose is about 30 times higher than at parenteral dose
• Distribution: Does not appear to cross the placental; is not secreted in breast milk; 15-25% bound to plasma protein
• Primary metabolsim: Hepatic; by cholinesterases
• Primary excretion: Kidneys
• Onset of Action: PO: 2-4 hrs; IM/IV: 10-30 mins
• Duration of action: t1/2: 50-90 mins

• due to its ability to stimulate the parasympathetic nervous system
• Common: involuntary contraction or twitching of muscles, N&V, miosis, and increased salivation.
• Potentially Serious: bradycardia, hypertension, dyspnea, and death due to paralysis of respiratory muscles

• used with caution in pts with disorders that could be aggravated by increased contractions o the GI tract, such as suspected bowel obstruction or active ulcers
• urinary obstruction, asthma and COPD,recent MI

• other cholinergic agnoists, drugs interfere with neuromuscular transmission, such as local anesthetics, some general anestheitcs, and antidysrhythmic agents,corticosteriods or NSAIDS
• herbal/food interactions: unknown

Category C

• Overdose is life threatening because it can cause respiratory failure
• Admin of atropine reverses most overdose symptoms

• monitor pulse, respiration, BP regularly (if below 60 contact physician)
• ensure atropine is available to restore heart rate or treat cholinergic crisis
• report onset of myasthenic symptoms (ocular motor disturbances, ptosis, diplopia, oropharyngeal muscle weakness, difficulty chewing, swallowing, or talking)

• take drug with milk or food to minimize gastric irritation
• be aware that regulation dosage interval is extremely difficult
• take larger portions of the total dose at times of greater fatigue
• certain times might increase size or frequency of dose (physical or emotional stress, infection, menstration, surgery)
• keep a diary of "peaks and valleys"
• immediately report: difficulty breathing, dizziness, difficulty moving, muscle cramps or spasms, slow or irregular heart beat, or vomiting
• wear a medic-alert braclet or other device describing your disease and details of medicatins

• Ambenonium (Mytelase)
• Edrophonium (Tensilon)
• Pyridostigmine (Mestinon)

• Therapeutic: Agent for bradycardia, antidote of muscarinic agonist overdose
• Pharmacologic: Anticholinergic, muscarinic antagonist

• increase heart rate
• relax smooth muscle in the GI, GU, and respiratory tracts
• decreases the quantity of exocrine secretions (suppress secretions of the salivary glands and respiratory tract during surgical procedures)
• topically to the eye: mydriasis and paraylyze the ciliary muscle, causing cyclaplegia (during eye exams)
• antidote used to reverse symptoms of toxicity due to overdose of cholineric angonists

• atropine blocks the parasympathetic activation by Ach and induces sympotms of the fight-or-flight response
• at high doses, the drug may block nicotinic receptors in the ganglias and on skeletal muscle

• Route(s): PO, IV, subcut, inhalation, or opthalmic
• Absorption: well absorbed by all routes
• Distributed; crosses the BBB and placenta; small amounts are in breast milk
• Primary metabolism: hepatic
• Primary excretion: Renal
• Onset of action: subcut/IM: 15 min; PO: 30 min; IV: 2-4 min
• Duration of action: t1/2: 2-3 hours

• drying of the oral and nasal mucosa, constipation, urinary retention, increased heart rate, blurred vision, photophobia
• serious: ventricular fibrillation, dilirium, and coma

• patients with acute angle-closure glaucoma
• safely has not been estabilished during pregnancy
• preexisting cardiopulmonary disease (COPD), MI, heart failure, HTN, hyperthyriodism, ulcerative colitis and illius, GERD, hiatal hernia experience decreased stomach emptying
• pts with Downs are sensitive due to structural differences in the CNS

• anticholinergic actions, such as antihistamines, tricyclic antidepressants, quinidine, and phenothiazines because their anticholenergic effects would be additive
• Herbal/Food: aloe, senna, buckthorn, and cascara sagrada may increase effects

Category C

• monitor VS, assess HR changes, rhythm, and quality, changes in RR, BP, temp
• observe of systemic changes with frequent or overuse of eye med
• Monitor I&Os, observe abd distention
• assess CNS status, can manifest drowsniess or stimulation
• monitor S&S of atropine fever (hyperpyrexia, due to suppression fo perspiration and heat loss) increased risk of heat stroke

• prevent or relieve dry mouth by drinking plenty of water; use small frequent mouth rinses; practice meticulous mouth and dental hygiene; chew sugarless gum or suck on hard candys
• use lubricating eye drops if eyes become dry and irritated
• increase fiber too prevent or correct constipation
• avoid driving
• do not breast-feed

• Antisecretory agents
• Antispasmodic agents
• Asthma agents
• Central acting agents
• Ophthalmic agents
• Scopolamine (Hyoscine, Transderm-Scop)
• Urge incontinence agents

• Therapeutic: Antihypertensive
• Pharmacologic: Ganglionic blocker, nicotinic receptor antagonist

• reduce BP (Rare)
• Tourette's syndrome
• treating cocaine and nicotine addictions

• A potent, long acting nicotinic receptor antagonist that blocks neurotransmission at both sympathetic and parasympathetic ganglia by competing with Ach for cholinergic receptor sites on postsynaptic membranes
• Readily crosses the BBB and inhibits the release of dopamine and NE

• Route(s): PO
• Absorption: Almost completely absorbed from the GI tract
• Distribution: Crosses the BBB and placenta; secreted in breast milk
• Primary metabolism: Hepatic
• Primary Excretion: Renal
• Onset of Action: 30 min-2 hrs
• Duration of action: 6-12 hrs

• weakness, fatigue, sedation, headache, mydriasis, blurred vision, decreased libido, impotence, urinary retention
• serious: orthostatic hypotension, precipitation of angina, choreiform movement, adynamic ileus

• impaired renal function
• coronary insufficiency, pyloric stenosis, glaucoma, recent MI, mild labile HTN, unreliable clients
• Herbal/Food: unknown

alcohol, bethanecho, thiazise diuretics, acetazolamide, sodium bicarb

Category C

treated with vasopressors

• Monitor VS, especially BP
• Assess for orthostatic hypotension
• Assess and report constipation, frequent loose stools with abd distention, or decreased bowel sounds

Position change slowly, lie down immediately if dizzy or light-headed, do not drive, relieve dry mouth with rinses, water, or hard candy, do not breast feed, never discontinue abruptly because it can result in severe rebound HTN

• Therapeutic: Skeletal muscle relaxant
• Pharmacologic: Neruomuscular blocker (depolarizing type)

first noted as muscle weakness and muscle spasms, then muscle paralysis occurs

binds to cholinergic receptors at neuromuscular junctions (nicotinic)

• Route(s): IM, IV
• Absorption: Well absorbed, IM
• Distribution: Completely, including crossing the placenta
• Primary metabolism: Plasma by pseudocholinesterase
• Primary Excretion: Renal
• Onset of Action: IV: less than 1 min; IM 2-3 min
• Duration of Action: IV: 2-3 min; IM: 10-30 min

• can cause complete paralysis of the diaphram and intercostal muscles, inhibit nerve transmission at ganglia causing tachycardia, hypotension, and urinary retention
• malignant hyperthermia
• respiratory depression, apnea, and dysrhythmias

hx of malignant hyperthermia, preexisting electrolyte imbalances, heart failure, pulmonary or metabolic disorders, kidney disease, glaucoma, children

Category C

• clindamycin, phemothiazine, aminoglycosides, furosemide, lithum, quinidine, lidocaine, anesthetics halthane or nitrous oxide, digoxin, opiods
• Herbal/Food: Melatonin

• Monitor VS
• Obtain baseline labs
• Monitor for transient apnea
• Prepare for emergency endotracheal intubation, articial respiration, and assisted or controlled respiration with O2
• sore throat and hoarseness are common
• report persistent muscle weakness

Succinlycholine is the only deporarizing neuromuscular blocker

• Therapeutic: Skeletal muscle relaxant
• Pharmacologic: Neuromuscular blocker (nondepolarizing)

skeletal muscle relaxation of paralysis

• competes with Ach for nicotinic receptor sites at motor end plates in skeletal muscle
• blocking nerve transmission to skeletal muscle prevents the muscles from contracting
• produces its effects without depolarizing the muscle cell membrane.
• drug will block Ach synapses at the ganglia at higher doses

• Route(s): IV
• Absorption: N/A
• Distribution: Completely distributed; does not cross the BBB; crosses the placenta
• Primary metabolism: Hepatic
• Primary Excretion: Renal; with smaller amounts in bile and feces
• Onset of action: 1 min
• Duration of action: t1/2: 1-3 hrs

• death due to paralysis of the respiratory muscles
• malignant hyperthermia (rare)
• bronchospasm, hypotension, muscle weakness, increased salivation

preexisting hyperthermia, preexisting electrolyte imbalances, heart failure, pt with acidosis, kidney disease

• drugs that block calcium channels or otherwise deplete calcium, including aminoglycoside and tetracycline antibiotics and calcium channel blockers
• procainamide, quinidine, clindamycin, amphotericin B, and diuretics
• Herbal/Food: Unknown

Category C

• drug is discontinued and assisted ventilation is provided until the effects of the drug wear off.
• Neostigmine may be administered to more rapidly reverse the neuromuscular blockade.
• Supportive therapy may be used to treat symptoms caused by histamine release

• Monitor VS
• Obtain baseline labs
• note selective muscle paralysis
• measure and record I&Os
• check for bowel sounds

report residual muscle weakness to the health care provider