Term
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Definition
| GI motility and secretion, release of urine, decrease HR and CO, Lower BP, Increase Salivation, Increase Bronchial secretions, Cause Miosis and contraction of ciliary muscle |
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Term
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Definition
| CNS, autonomic ganglia, adrenal medulla, and neuromuscular junctions |
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Term
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Definition
| , Increase PVR, cause urinary retention, increase BP, Mydriasis |
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Term
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Definition
| inhibit release of NE, Ach, and insulin |
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Term
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Definition
| , Increase cardiac contraction, increase lipolysis and release of rennin |
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Term
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Definition
| Vasodilation, decrease PVR, bronchodilation, release of glucagon, glycogenolysis, relax uterine smooth muscle |
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Term
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Definition
| by Acetylcholinesterase hydrolyzing Ach into choline and Acetyl Co-A |
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Term
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Definition
| Methylated by COMT in post synaptic and oxidized by MOA in the neuron. Taken back up into the neuron or metabolized |
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Term
| Cholinergic agonist actions |
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Definition
| Mimic the effects of ACH. Parasympathomimetic. Act on muscarinic and nicotinic receptors and stimulate effects of Ach like GI motility, urinary excretion, and decreasing IOP. Two groups are Choline esters which are Ach and synthetic like carbachol and Bethanachol. Naturally occurring alkaloids are pilocarpine |
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Term
| Cholinergic Indirect agonist activity |
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Definition
| Inhibit the reuptake of Ach by binding to Achesterase |
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Term
Cholinergic Antagonist activity
Muscarinic and Nicotinic
NMB antagonists and agonists |
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Definition
Muscarinic blockers block the neurotransmitter from binding to the muscarinic receptor
Nicotinic:
Ganglionic: Work by binding to nicotinic receptors on the autonomic nervous system blocking the output of the ANS
NMB drugs: Inhibit the transmission of Ach at the end of nerves and the nicotinic receptors at the end plate of skeletal muscle
Antagonists: non-depolarizing and don’t allow Ach to bind. Ex: is Tubocurarine
Agonists- Depolarizing and allow Ach to bind causing muscle twitches but eventual paralysis. Ex: is Succinylcholine |
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Term
| Action and Uses for Bethanechol |
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Definition
MoA- Muscarinic activity and increases GI motility and GU/expulsion of urine
Uses: Post op abdominal distension or urinary distension. Not destroyed by Achesterase |
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Term
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Definition
| SE: Sweating, salivation, flushing, low BP, nausea, ab pain, diarrhea, bronchospasm |
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Term
| Carbachol action and uses |
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Definition
MoA- Nicotinic and muscarinic actions Resistant to Achesterase
Uses- highly potent and long duration limit the uses. Used locally in eye for miosis, good for decreasing intraocular pressure like in glaucoma |
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Term
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Definition
| Little SE because little systemic absorption because used in the eye |
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Term
| Pilocarpine action and use |
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Definition
MoA: Resistant to Achesterase and muscarinic activity. When applied to eye causes miosis and contraction of ciliary muscle. Promote salivation
Uses: Lower intraocular pressure and drain aqueous humor, also for xxerostomia |
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Term
| Physostigmine action and uses |
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Definition
MoA: Lasts 2-4 hours, intermediate action and may enter CNS. Binds with Achesterase and inhibits the destruction of Ach
Uses: increase intestinal and bladder mobility, cause miosis of eye, MAINLY used for treatment of overdoses of drugs with anticholinergic actions like atropine |
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Term
| Physostigmine action and uses |
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Definition
MoA: Lasts 2-4 hours, intermediate action and may enter CNS. Binds with Achesterase and inhibits the destruction of Ach
Uses: increase intestinal and bladder mobility, cause miosis of eye, MAINLY used for treatment of overdoses of drugs with anticholinergic actions like atropine |
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Term
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Definition
| SE: convulsions, bradycardia, skeletal muscle paralysis |
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Term
| Neostigmine actions and uses |
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Definition
MoA: Synthetic inhibitor of Achesterase and has less CNS penetration. Greater effect on muscles
Uses: lasts ½ to 2 hours and used to stimulate bladder and GI tract also an antidote for tubocurarine. Used for Myasthenia Gravis |
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Term
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Definition
| SE: Salivation, decrease BP, flushing and nausea, ab pain, diarrhea, bronchospasm |
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Term
| Pyridostigmine and ambenomium |
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Definition
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Term
| Demcarium and edrophonium |
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Definition
| Indirect chol aganoist for open and closed angled glaucoma and used for accommodative esotropia |
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Term
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Definition
Irreversible covalent binding, toxic, in nerve gas and insecticides
Echothiophate
PERMANENTLY inactivates Ach causing paralysis of motor function, convulsions, miosis |
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Term
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Definition
| PERMANENTLY inactivates Ach causing paralysis of motor function, convulsions, miosis |
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Term
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Definition
MoA: causes mydriasis of eye, cycloplegia, cause an increase in IOP, used in eye exams but shorter acting preferred. Slows down Gi activity but HCL no inhibited Decrease motility of bladder Used in enuresis for pediatrics Block salivary glands and decrease sweat and lacrimation
Uses: Ophthalmic: see refractive errors. Antispasmodic and relaxes muscle of GI. Antisecretory and block secretion in upper and lower respiratory tract Low doses used to overcome toxicity symptoms |
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Term
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Definition
| SE: xerostomia, blurred vision, irritated eyes, tachycardia, constipation, CNS confusion |
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Term
| Muscarinic antagonist drugs |
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Definition
| Atropine, scopolamine, Ipratropium, tropicamide and cyclopentolate |
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Term
| Scopolamine action and use |
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Definition
MoA: peripheral effects same as atropine more effect on CNS and longer duration.
Uses: PREVENTION OF MOTION SICKNESS, used in anesthesia to prevent nausea and vomiting |
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Term
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Definition
Uses: inhaled for help in COPD and 2nd line for asthma
SE: local action and lack of CNS penetration there are few SE |
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Term
| Tropicamide and cyclopentolate |
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Definition
Uses: Ophthalmic conditions similar to atropine but shorter duration
Competitive muscarinic receptor antagonists
Uses: overactive bladder |
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Term
| Nicotinic anatagonist non depolarizing drug |
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Definition
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Term
| Tubocururainie action and use |
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Definition
MoA: Compete at binding site for Ach. Overcome by increasing aceytlcholine
Used to decrease amount of anesteshia needed. Less anesthetic se and quicker recovery |
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Term
| non depolarizing nicotinic antagonist low dose and high dose effects |
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Definition
Low doses: Interact with nicotinic receptors and prevent binding of Ach
High doses: block ion channels and weaken neuromuscular tansmission, reduce ability of cholinesterase inhibitors. Small fast twitch muscles like in eyes and face are more receptive to non deporizers and more paraylysis then eyes, then limbs, intercostals, and last is diaphragm. Some can cause release of histamine
Uses: Adjunct in anesthesia. Relax skeletal muscle, facilitation of intubation, Orthopedic surgery
SE: Adverse Effects, Tubocurarine (rarely used due to AEs), Histamine release & ganglionic blockade |
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Term
| Depolarizing NMB action and use |
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Definition
Succinylcholine
Attached to nicotinic receptor and acts like Ach depolarizing the junction
Depolarization or opening of Na channels cause twitching of muscles and continued binding causes receptors unable to transmit further impulses. Also can lead to gradual repolarization which causes resistance to depolarization
Actions: Sequence of paralyzing action can vary but respiratory are paralyzed last, short period of muscle twitches then paralysis and short duration and rapid onset
Uses: rapid endotracheal intubation, given IV |
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Term
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Definition
| SE: hyperthermia, apnea if deficit of plasma cholinesterase, hyperkalemia because increases potassium release from intracellular stores |
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Term
| Adrenergic Direct Agonists Actions and drugs |
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Definition
Direct agonists
MoA: Act directly on alpha or beta receptors. Produce similar effects of epinephrine.
Drugs: Epinephrine, norepinephrine, isoproterenol, phenylephrine |
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Term
| Adrenergic indirect agonists and drugs |
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Definition
MoA: Block reuptake of Ne
Drugs: cocaine, TCA’s, Amphetamines |
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Term
| Mixed adrenergic agonists action and drugs |
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Definition
MoA: Stimulate adrenoreceptors directly and release NE from the adrenergic neurons
Drugs: Ephedrine and pseudoephedrine |
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Term
| Epinephrine action Cardiac and respiratory |
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Definition
MoA: Direct adrenergic agonist and naturally occurring catecholamine. Interacts with both alpha and beta Low doses with beta and vasodilation High doses alpha and vasoconstriction
Cardiac: Beta 1 effects increase heart contraction and rate
Alpha effects cause constriction of arterioles in skin, mucous membranes and viscera and decrease renal blood flow
Respiratory: Beta 2 effects and cause bronchodilation, relieves bronchoconstriction due to allergies or histamine |
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Term
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Definition
Uses: bronchospasm/anaphylactic shock. FIRST CHOICE for type 1 hypersensitivity allergic reactions –(EpiPen) acute asthma, and chronic asthma
Glaucoma- applied topically to reduce IOP and decrease prod. Of aq hum.
Cardiac Arrest
Local anesthetics- increase DoA by vasoconstriction allowing anesthetic to stay at site of action longer and used to constrict vessels for suturing to decrease the bleeding |
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Term
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Definition
| SE: CNS disturbance- anxiety, headache, cerebral hemorrhage, cardiac arrhythmias, pulmonary edema, hyperglycemia |
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Term
| Norepinephrine Action and cardiac effect |
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Definition
MoA: alpha receptors stimulated
Cardiac- vasoconstriction and baroreceptor reflex |
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Term
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Definition
| Uses: Shock to increase BP by increasing vascular resistance |
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Term
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Definition
| SE: Similar to epi, blanching and sloughing of skin at injection site |
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Term
Isoproterenol MoA
Cardiac and pulmonary |
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Definition
MoA: direct adrenergic agonist and synthetic catecholamine. Stimulation of beta 1 and 2
Cardio: B1 Cells and Pulmonary is B2 cells causing bronchodilation. Given paraentral so inhaled or through buccal muscosa |
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Term
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Definition
| Uses: Stimulation of heart in emergencies less likely used for asthma |
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Term
Dopamine MoA
Cardiac and renal |
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Definition
precursor of NE
MoA: activates alpha and beta, high doses is alpha 1 vasoconstriction, low dose is beta 1 cardiac stimulation
Cardio: beta 1 has inotropic (contraction force) and chronotropic (rate and rhythm) effects and vasoconstriction at high dose
Renal and visceral: dilate renal arterioles
Uses: for shock by increasing BP from stimulation of beta 1 receptors on heart and alpha 1 receptors but increase blood to kidney as well |
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Term
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Definition
| Uses: for shock by increasing BP from stimulation of beta 1 receptors on heart and alpha 1 receptors but increase blood to kidney as well |
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Term
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Definition
| SE: overdose same effects as sympathetic stimulation but don’t last long |
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Term
Other agonists
Dobutamine, Oxmetazoline, Phenylephrine, Clonidine, Metaproterenol, Albuterol, Salmeterol and formoterol |
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Definition
Dobutamine
Synthetic beta 1 agonist used to increase cardiac output
Oxmetazoline
Direct alpha 1 2 agonist used in eye or nose for vasoconstriction. Afrin
Phenylephrine
Direct synthetic alpha 1 not a catecholamine used for nasal congestion and mydriosis also used to elevate BP. Sudafed PE
Clonidine
Central alpha 2 used for hypertension
Metaproterenol
Like isoproterenol but not catecholamine, inhalation for asthma
Albuterol
Short acting beta 2 for bronchodilation, used for asthma, less cardiac
Salmeterol and formoterol:
Long acting beta 2 for bronchodilation but delayed onset, used with other medications for asthma |
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Term
| Alpha Adrenergic Blockers |
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Definition
Blood Pressure! Alpha 1 antagonists block the sympathetic effects on BP and decrease peripheral vascular resistance.
Phenoxybenzamine, phentolamine |
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Term
| Phenoxybenzamine action and cardiac effect |
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Definition
MoA: non selective alpha blocker, irreversible and noncompetitive
Cardio: prevents vasoconstriction of peripheral blood vessels, increases NE release and stimulation of Beta receptors, not successful in treating HTN |
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Term
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Definition
| Uses: Pheocromocytoma also raynauds disease which is vasoconstriction in extremeties and autonomic hyperreflexia which is an autonomic nervous response |
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Term
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Definition
| SE: orthostatic hypotension, nasal congestion, nausea/vomiting, tachycardia. Don’t use with decreased coronary perfusion |
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Term
| Phentolamine action and uses |
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Definition
MoA: competitive blockade of alpha 1 and 2. Lasts 4 hours
Uses: Short term management of pheochromocytomas and reverses effects of epinephrine, also used for ed |
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Term
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Definition
| SE: causes orthostatic hypotension, arrhythmias, and chast pain |
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Term
Selective competitive alpha 1 blockers
MoA for cardio and prostate |
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Definition
MoA: Cardio- decrease BP and PVR relax arterial and venous smooth muscle
Drugs: Prazosin, terazosin, doxazosin for HTN
Prostate- improves urine flow by decreasing tone of smooth muscle in bladder and prostate improves urine flow
Drugs: flomax, alfuzosin for BPH less effect on BP more on prostate |
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Term
| Selective competitive Alpha 1 blocker SE and interactions |
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Definition
SE: tolerance, 1st dose response so exaggerated orthostatic hypotension causing syncope so give before bed or less dosage, CNS dizziness
Interactions: Additive antihypertensive effects with diuretic or beta blocker and prazosin can cause fluid retention |
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Term
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Definition
| Competitive antagonists and block beta 1 and 2 receptors. Cardio blocks beta 1 lowering bp but alpha receptors still functional so no postural hypotension. Symp control of vasculature maintained, no useful B2 antagonists |
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Term
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Definition
| Propranolol, Timolol, and Nadolol |
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Term
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Definition
MoA: Cardio- B1 decreases cardiac output, - inotrope and chronotrope, direct suppression of SA and AV activity and decrease cardiac output and workload as well as cardiac oxygen
Peripheral vasoconstriction- prevent B2 mediated vasodilation, reduction in cardiac output leads to less BP and this causes peripheral vasoconstriction
Bronchoconstriction- block B2 in the lungs but contraindicated in COPD and asthma
Na retention- decrease in BP and renal perfusion causes increase in Na retention and plasma volume
Hypoglycemia- careful monitoring in DM BB decreases glycogenolysis and decreases glucagon secretion |
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Term
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Definition
Uses: Hypertension, Glaucoma decreasing aq hum secretion not affecting pupil size, also migraine prophylaxis by decreasing intensity and frequency blocking catecholamine induced vasodilation
Hyperthyroidism- blunts sympathetic stim and protects against cardiac arrhythmias
Angina Pectoris- chronic management of stable angina by decreasing cardiac workload
MI- protects myocardium and decreases infarct size hastening recovery |
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Term
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Definition
SE: Bronchoconstriction- serious in asthma or COPD patients, arrhythmias if abrupt discontinuation, hypoglycemia and sexual dysfunction
Drug interactions: cyp 450 |
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Term
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Definition
Timolol- used in eye to decrease aqueous humor production
Nadolol- long duration used for HTN |
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Term
| Cardioselective B Blockers MoA and uses |
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Definition
MoA- block Beta 1 and minimize bronchoconstrictor effects, decrease BP and improve exercise tolerance
Uses: HTN, heart failure, prevention of secondary MI used in DM and pulmonary dysfunction pts |
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Term
| Actions and use of Antagonist and partial agonist activity on Beta |
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Definition
weak stimulation of B1 and B2. Inhibits action of epi and norepi, intrinsic sympathomimetic
Uses: BB with ISA’s is good for hypertension with moderate badycardia,
Drugs are pindolol and acebutolol |
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Term
| Antagonists of Alpha and Beta actions and uses |
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Definition
Actions: reversible B blockade and Alpha 1 blocking actions for peripheral vasodilation
Uses: Hypertension, esp. patients which increase PVR isn’t wanted |
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Term
| SE of A and B antagonists |
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Definition
| SE: orthostatic hypotension and dizziness |
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Term
| Drugs affecting NT release or uptake |
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Definition
Reserpine
Impaired sympathetic function due to decrease of NE blocks transport of amines in vesicles
Guanethidine
Blocks release of stored NE leads to gradual depletion of NE in nerve endings |
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