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Pharm 18-19
Adrenergics and blockers; Cholinergics and anti
Question | Answer |
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Cholinergics (definition) | drugs that stimulate the parasympathetic nervous system; mimic the parasympathetic neurotransmitter acetylcholine |
Acetylcholine (ACh) | neurotransmitter located in the ganglions and the parasympathetic terminal nerve endings; innervates the receptors in organs, tissues, and glands |
Types of cholinergic receptors (2) | muscarinic receptors - stimulate smooth muscle and slow the heart rate nicotinic receptors - neuromuscular; affect skeletal muscles |
Selective vs nonselective | selective - affect muscarinic but do NOT affect nicotinic receptors nonselective - affect BOTH muscarinic and nicotinic receptors |
Direct-acting cholingeric drugs | act on the receptors to activate a tissue response; selective to muscarinic receptors; located in smooth muscle; heart, GI, GU, glands |
Indirect-acting cholinergic drugs | inhibit the action of cholinesterase by forming a chemical complex, thus permitting aceytlcholine to persist and attach to the receptor; reversible - binds for several minutes to hours; irreversible - bind permanently; stimulates skel muscles, inc tone |
Anticholinesterase drugs (definition) | drugs that inhibit cholinesterase; more acetylcholine is available |
Effects of cholinergic drugs: cardiovascular | decreases heart rate, lowers BP (vasodilation), slows conduction of atrioventricular node |
Effects of cholinergic drugs: gastrointestinal | increases tone and motility of smooth muscles of stomach and intestine, peristalsis is increased and sphincter muscles are relaxed |
Effects of cholinergic drugs: genitourinary | contracts muscles of the urinary bladder, increases tone of ureters, and relaxes bladder's sphincter muscles; stimulates urination |
Effects of cholinergic drugs: ocular | increases pupillary constriction, or miosis (pupils become smaller), and increases accomodation |
Effects of cholinergic drugs: glandular | increases salivation, perspiration, and tears |
Effects of cholinergic drugs: bronchial (lung) | stimulates bronchial smooth muscle contraction and increases bronchial secretions |
Effects of cholinergic drugs: striated muscle | increases neuromuscular transmission and maintains muscle strength and tone |
Bethanechol chloride (prototype; class; contraindications; interactions) | cholinergic/parasympathomimetic Trade name: Urecholine, Duvoid Contraindications: severe bradycardia or hypotension, COPD, asthma, peptic ulcer, parkinsonism, hyperthyroidism Drug interactions: decreased effect with antidysrhythmics Lab: inc AST, bili |
Bethanechol chloride (prototype; theraputic effects; mode of action) | Use: to treat urinary retention, abdominal distention Mode of action: stimulate the cholinergic (muscarinic)receptor; promote contraction of the bladder; increase GI peristalsis, GI secretion, pupillary constriction, and bronchoconstriction |
Bethanechol chloride (prototype; side effects and adverse reactions) | nausea, vomiting, diarrhea, salivation, sweating, flushing, frequent urination, rash, miosis, blurred vision, abdominal discomfort Adverse: orthostatic hypo, bradycardia, muscle weakness, heart block, circulatory collapse, cardiac arrest, acute asthmatic |
Bethanechol chloride (prototype; nursing interventions) | measure I & 0, urinal at bedside, BP, pulse, get up slowly, breath sounds, give 1 hr before meals or 2 hrs after; OD = atropine |
Anticholinergics (parasympatholytics) | inhibits the action of acetylcholine by occupying the acetylcholine receptors; heart, respiratory tract, GI tract, urinary bladder, eyes, exocrine glands |
Effects of anticholinergic drugs: cardiovascular | increases heart rate with large doses; small doses can decrease heart rate |
Effects of anticholinergic drugs: gastrointestinal | relaxes smooth muscle tone of GI tract, decreasing GI motility and peristalsis; decreases gastric and intestinal secretions |
Effects of anticholinergic drugs: urinary tract | relaxes the bladder detrusor muscle and increases constriction of the internal sphincter; urinary retention can result |
Effects of anticholinergic drugs: ocular | dilates pupils and paralyzes ciliary muscle, causing a decrease in accommodation |
Effects of anticholinergic drugs: glandular | decreases salivation, perspiration, and bronchial secretions |
Effects of anticholinergic drugs: bronchial | dilates the bronchi and decreases bronchial secretions |
Effects of anticholinergic drugs: CNS | decreases tremors and rigidity of muscles; drowsiness, disorientation, and hallucinations can result from large doses |
Atropine (prototype; class; contraindications; route) | anticholinergic/parasmupatholytic Trade: Atropine, Atropisol (optic), Atropair Contraindications: narrow-angle glaucoma, obstructive GI disorders, paralytic ileus, ulcerative colitis, tachy, benign prostatic hypertrophy, MG, myocardial ischemia; IV or |
Atropine (prototype; interactions; use; mode of action) | Drug inter: inc effect c phenothiazines, antihistamines, tricyclic antidepressants Use: preoperative medication to reduce salivation, increase heart rate and dilate pupils Mode: occupy receptors; increase HR by blocking vagus; block spincter dilate pupi |
Atropine (prototype; side effects and adverse reactions) | Side effects: dry mouth, naus, headache, constipation, rash, dry skin, flush, blurred vision, photophob, urinary retention Adverse: tachy, hypotension, pupil dilation, ab distension, palpitations, nasal congest, paralystic ileus, coma |
Atropine (protoype; nursing interventions) | heart rate - vitals; I & O; bowel sounds; oral care; eye drops; avoid hot environments; avoid alcohol, caffeine, aspirin in PM, cigarettes |
Triexyphenidyl HCL (prototype; class; contraindications) | antiparkinson: anticholinergic agent Trade: Artane, Trihexane, Trihexy, Aparkane, Apo-Trihex, Novohexidyl Contra: glaucoma, GI obstruction, urin retention, severe angina pectoris, MG (Caution: tacy, children/elderly, nursing mothers) |
Triexyphenidyl HCL (prototype; interactions; route) | Drug: increased effect c phenothiazines, antihistamines, tricyclic antidepressants, amantadine, quinidine; decreased effect c antacids Route: PO |
Triexyphenidyl HCL (prototype; uses; mode of action) | Uses: to decrease involuntary symptoms of parkisonism or drug-induced parkinsonism by inhibiting acetylcholine Mode: blocks cholinergic (muscarinic) receptors to decrease involuntary movements |
Triexyphenidyl HCL (prototype; side effects and adverse reactions) | Side effects: naus, vomit, dry mth, consti, anxiety, restlessness, hdache, flushing, dizzi, blurred vision, photophobia, pupil dilation, dysphagia Adverse: tachy, palp, urticaria, postural hypotn, urinary rtn |
Antihistamine/anticholinergics | treats motion sickness Side effects: dry mouth, visual disturbances, constipation, urinary rtn, flushing, muscle weakness, tachy, hypotension, drowsiness |
Tolterodine tartrate (prototype; class, contraindications) | Antimuscarinic agent: anticholinergic Trade: Detrol (LA) Contra: allergies, urinary rtn, gastric rtn, uncontrolled glaucoma Caution c: controlled glaucoma, CV disease, urinary bladder outflow obstruc, pyloric stenosis, lactation, renal of hepatic dysfu |
Tolterodine tartrate (prototype; drug interactions) | Increased effects c: tricyclic antidepressants and many others.. Decreased effects c: antifungals, antubiotics |
Tolterodine tartrate (prototype; use, mode of action) | Uses: to decrease urinary frequency, urgency and incontinence Mode: blocks cholinergic (muscarinic) receptors selectively in urinary bladder |
Tolterodine tartrate (prototype; side effects and adverse reactions) | Side: dry mouth and eyes, headache, dizzi, fainting, nervous, naus, vomit, diarrhea, ab pain, dyspepsia, flatulence, dysuria, weight gain, arthralgia, urinary rtn, UTI, URI, rash, itching, dry skin Adverse: bronchitis, visual abnormal, chest pain, HTN |
Adrenergics (definition) | stimulate the sypathetic nervous system; mimic symathetic neurotransmitters; "fight or flight" |
Effects of adrenergics at receptors: Alpha 1 | increases force of heart contraction; vasoconstriction increases BP; dilation of pupils; salivary glands decrease secretion; increases urinary bladder relaxation and urinary sphincter contraction; in vessels of muscle |
Effects of adrenergics at receptors: Alpha 2 | inhibits release of norephinephrine; dilates blood vessels; produces HTN; decreases GI motility and tone; located in vessels in muscle |
Effects of adrenergics at receptors: Beta 1 | increases heart rate and force of contraction; increases renin secretion, which increases BP; located in the heart |
Effects of adrenergics at receptors: Beta 2 | dilates bronchioles; promotes GI and uterine relaxation; promotes increase in blood sugar thru glycogenolysis in liver; increases blood flow in skeletal muscles; located in lungs |
Epinephrine (prototype; class; contraindications) | symathomimetic Trade: Adrenalin Contra: cardiac dysrhythmias, cerebral ateriosclerosis, pregnancy, glaucoma, cardiogenic shock (CAUTION: HTN, prostatic hypertrophy, hyperthyroidism, pregnancy, diabetes |
Epinephrine (prototype; interactions) | Drug: decreases effect c methyldopa, beta blockers, alpha adrenergic blockers Lab: increase blood glucose, serum lactic acid |
Epinephrine (prototype; uses; mode of action) | Uses: to treat allergic reactions, anaphylaxis, bronchospasm,cardiac arrest Mode: action on one or more adrenergic sites; promotion of CNS and cardiac stimulation and bronchodilation; nonselective |
Epinephrine (prototype; side effects and adverse reactions) | Side: anorexia, naus, vomit, nervousness, tremors, agitation, headache, pallor, insomnia, syncope, dizziness Adverse: palp, tachy, dyspnea, v fib, pulmonary edema |
Epinephrine (prototype; nursing interventions) | monitor: BP, pulse, respirations, vitals q5min, urine output (catheter), glucose levels Avoid: caffeine, breastfeeding, nasal sprays with ephinephrine |
Albuterol (prototype; class; contraindications; use; mode) | beta2-adrenergic agonist Trade: Proventil Conta: none (Caution: severe cardiac disease, HTN, hyperthyroid, diabetes, preg) Use: treat bronchospasm, asthma, bronchitis, COPD Mode: stimulates beta2, relaxes bronchial smooth muscle; selective |
Albuterol (prototype; lab interactions; side effects and adverse reactions) | Lab: may increase glucose and decrease serum K Side: tremor, dizzi, nervous, restlessness Adverse: palp, reflex tachy, hallucinations, cardiac dysrhythmias |
Dopaminergics | located in renal, mesenteric, coronary, and cerebral arteries; vessels dilate and blood flow increases; only dopamine can activate; increases BP without deceasing renal function |
Albuterol (prototype; drug interactions) | may increase effect with other sympathomimetics, MAO inhibitors and tricylic antidepressants (antiparkinson and antipsychotics); antagonizes effect with beta blockers |
Adrenergic blockers (definition) | blocks the effect of adrenergic neurotransmitters; blocks alpha and beta receptor sites; occupies the receptor sites; indirectly by inhibiting release of neurotrasmitters ephinephrine and norepinephrine |
Effects of adrenergic blockers: Alpha 1 | vasodilation: decreases blood pressure; reflex tachycardia might result; miosis occurs; suppresses ejaculation; reduces contraction of smooth muscle in bladder neck and prostate gland |
Effects of adrenergic blockers: Beta 1 | decreases heart rate; reduces force of contractions |
Effects of adrenergic blockers: Beta 2 | constricts bronchioles; contracts uterus; inhibits glycogenolysis, which can decrease blood sugar |
Neurotransmitter inactivation | once it has accomplished its job, must be inactivated to prevent prolonged effect; reuptake, degradation by enzymes, diffusion away from receptor |
Alpha-adrenergic blockers (definition) | uses: treat peripheral vascular disease (Raynaud's) and benign protstatic hypertrophy (BPH); can cause orthostatic hypotension; cause vasodilation in periphery and decrease in BP |
Beta-adrenergic blocks (definition) | AKA beta blockers; decrease HR, decrease BP, bronchoconstriction occurs; treats - angina, dysrhythmias, HTN, heart failure |
Atenolol (prototype; class; contraindications) | beta1-adrenergic blocker Trade: Ternormin Contra: sinus brady, heart block, cardiogenic shock, overt cardiac failure (CAUTION: renal dys, peripheral arterial circ disorders, asthma, COPD, hyperthyroidism, use of diuretics and digitalis) |
Atenolol (prototype; drug interactions) | Drug: increased absorption c atropine and other anticholinergics, decreased effects c NSAIDs, increased risk of hypoglycemia c insulin and sulfonyureas, increased hypotension |
Atenolol (prototype; uses; mode of action) | Uses: to treat HTN, angina pectoris, and myocardial infarction Mode: selectively blocks beta1-adrenergic receptor sites, decreases sympathetic outflow to the periphery, supresses renin-angiotensin-aldosterone system |
Atenolol (prototype; side effects and adverse reactions) | Side: drowsiness, dizzi, fainting, depression, weakness, naus, vomit, diarrhea, cool extremities, leg pain Adverse: brady, hypotension, heart failure, masking of hypoglycemia, pulmonary edema, dysrhythimias |
Adreergic neuron blockers | block the release of norepinephrine; subdivision of adrenergic blockers; used to decrease BP gradually; get baseline vitals and EKG; Ex - reserpine (Serpalan) |
St. John's Wort | may antagonize hypotensive effects of resperine (adrenergic neuron blocker) |