Drugs affecting Autonomic Nervous System Flashcards

Question

Postsynaptic adrenergic receptor stimulation: Effects of Beta-2

Answer 1

* bronchodilation, * vasodilation, * GI relaxation, * uterine relaxation, * glycogenolysis (hyperglycemia)

Answer 2

Alpha-2 and Beta-2

Answer 3

Alpha-2 and Beta-2

Answer 4

•Mydriasis (dilate eyes for eye exam)

Answer 5

•Cause bronchodilation and manage anaphylactic shock

Answer 6

•Improve myocardial contractility, increase in heart rate and blood pressure

Answer 7

Decrease peristalsis

Answer 8

Increases blood sugar

Answer 9

Prolongs anesthetic action

Answer 10

Fear Restlessness Headache Tremor Palpitations Pallor Serious ADRs Stroke V-Fib

Answer 11

Stimulation of Alpha2 receptors creates a negative feedback loop and inhibits sympathetic outflow (aka sympatholytic).

Answer 12

Dry mouth Constipation Nausea GI Upset

Answer 13

Similar to parasympathetic effects: Bradycardia Hypotension (Impotence)

Answer 14

Receptor: Selective Alpha-1 Agonist Action: Vasopressor Uses: Treat congestion, hypotension, (uveitis)

Answer 15

MOA: Causes vasodilation by stimulating inhibitory alpha-adrenergic receptors in the brain (centrally)

Answer 16

Lowers blood pressure (2nd or 3rd line) and heart rate Used for treatment of withdrawal symptoms (ETOH, nicotine, heroin) Used for attention deficit hyperactivity disorder

Answer 17

Sedation, dry mouth, and postural hypotension occur but these usually decrease after several weeks of therapy. Sodium and water retention may occur. Bradycardia, Skin rashes, constipation, urinary retention, impotence, and nightmares may occur. Abrupt discontinuation of clonidine can result in Rebound Hypertension as soon as 8 and as late as 36 hours after the last dose. Gradually taper over 4 days

Answer 18

Caution in elderly because they are at risk for orthostatic hypotension and fluid retention. Cat C Pregnancy

Answer 19

Abrupt discontinuation of clonidine can result in Rebound Hypertension as soon as 8 and as late as 36 hours after the last dose. Gradually taper over 4 days.

Answer 20

Sedation, **_hepatotoxicity_** (elevations of transaminase enzymes; fever, malaise & jaundice may occur), **_development of a positive Coomb's test_** (in 10-20% of patients taking 1 g daily for \> 6 mo; hemolytic anemia does not occur), flu-like symptoms. Retention of sodium and weight gain may occur during treatment. Abrupt discontinuation can result in rebound hypertension as soon as 8 and as late as 36 hours after the last dose. Gradually taper over 4 days Coombs test info: The direct Coombs test is used to test for autoimmune hemolytic anemia; i.e., a condition of a low count of red blood cells (a.k.a. RBCs) caused by immune system lysis or breaking of RBC membranes causing RBC destruction.

Answer 21

* Receptor: Beta-1 * Use: Cardiac Decompensation * ADR: Increases heart rate and blood pressure; angina

Answer 22

* Relatively selective Beta-2 agonist * Use: Bronchodilation

Answer 23

•CNS stimulation, * palpitation, * tremors , * shakiness , * hyperactivity , * headache , and * nausea & vomiting . * May cause irritable behavior in infants

Answer 24

* Clinical use in adults and children as young as 4 y/o * Rational drug selection: Caution: Patients at risk include diabetics, hyperthyroidism, subjects with seizures disorders, and the elderly. * Excessive use may cause death, cause unknown but probably cardiac arrest. Oral use may delay preterm labor.

Answer 25

Receptors: Alpha 1 & 2; Beta 1 & 2 Uses * Prolong local anesthetics * Treat allergic reactions * CPR * Status Asthmaticus

Answer 26

* Receptors: Alpha 1; Less Beta 1 * Uses: Treat hypotension

Answer 27

* Receptors: Dopamine; Beta-1; Alpha 1 (dose dependent) * Causes: Renal Vasodilation; Stimulates heart * Use: Shock syndrome * ADR: Palpitations, hypotension

Answer 28

* Pseudoephedrine (Sudafed) * Receptors: Alpha & Beta-2 * Uses: Decongestant * Amphetamine/ Methylphenidate (Ritalin) * Receptors: Direct and Indirect Adrenergic * Uses: ADHD; Narcolepsy * ADR: Nervousness, Insomnia, arrhythmias, tachycardia, headache * Warnings: HBP; CAD; Glaucoma; Hyperthyroidism; BPH, DM

Answer 29

"blockers"

Answer 30

* Action: block alpha receptors leading to vasodilation * Used to treat HTN, benign prostatic hyperplasia (BPH), Raynaud’s disease, and migraine headaches * Nonselective (Phentolamine (Regitine)) * Selective Alpha-1- see next slide

Answer 31

* Action: antagonize or block the effects of catecholamines (epi, NE, dopa); decreases heart rate and reduces vascular smooth muscle tone/ resistance * Drugs can be “selective” to beta1 receptors or “nonselective” to beta1 and beta2 receptors * Mainly used for HTN and post myocardial infarction (MI)

Answer 32

"-zosin" Example: * Prazosin (Minipress), * Doxazosin (Cardura), * Terazosin (Hytrin) * Used for HTN * Tamsulosin (Flomax): Used for BPH

Answer 33

Fluid retention, Orthostatic HTN (plus dry mouth, constipation, urinary retention, etc) **Warning: 1st dose effect** _excess postural hypotension that can occur within 30-90 min of the first few doses_ The patient will adjust to the medication with successive doses To avoid: Take at bedtime; start at 1mg and titrate up every 2 weeks Way to remember- That patient is “dozin” on the floor! Orthostatic hypotension is a side effect of “zosin”.

Answer 34

Nonselective: Blocks beta-1 and beta-2 (e.g., propranolol [Inderal]) ( 1st generation)

Answer 35

Selective for beta-1 receptors (e.g., metoprolol [Toprol]) and atenolol [Tenormin]) : relatively “cardioselective” beta-1 antagonists) (2nd generation)

Answer 36

Combined Beta blockers (nonselective) with alpha blocking activity: (e.g., **labetalol** [Normodyne]) & **carvedilol** [Coreg]): _Used to **reduce the progression on heart failure** because they cause vasodilation of the peripheral vasculature_; Especially effective in African Americans

Answer 37

Dizziness, lethargy/ fatigue, nightmares, mental status changes in elderly, impotence

Answer 38

bradycardia, reduced cardiac output precipitation of heart failure AV heart block and rebound cardiac excitation (however they are 1st line drugs in certain types of heart failure, given in left ventricular dysfunction).

Answer 39

bronchoconstriction and hypoglycemia | (from inhibition of glycogenolysis)

Answer 40

Upregulation of Beta-1 receptors.

Answer 41

DO NOT STOP ABRUPTLY (life threatening especially in pts with angina and CAD) Acute discontinuation of beta blockers can result in excess sympathetic activity seen in 24-48 hours, due to an increase in beta receptors (up-regulation) during blockade. Myocardial ischemia or cardiac arrhythmias may occur. Can be minimized by withdrawing these drugs gradually (decrease dose by a half every 4 days- can take 1 to 2 weeks). Contraindicated: (Esp. non-selective) Asthma or any bronchospastic condition, **_Caution in diabetics- masks hypoglycemic symptoms EXCEPT diaphoresis)_**, Avoid in pregnant & nursing women

Answer 42

In renal impaired pts be sure to extend the dosage interval. There is a higher risk of toxicities if the dosing interval is inadequate to allow for drug elimination.

Answer 43

parasympathomimetics, muscarinic agonists

Answer 44

◦Prototype: bethanechol (Urecholine) ◦Prototype: pilocarpine (Pilocar)

Answer 45

◦Cholinesterase inhibitors ◦Peripheral-Acting: Prototype: neostigmine bromide (Prostigmin) ◦Central-Acting: Donepezil (Aricept)

Answer 46

Muscarinic agonists act directly on postganglionic parasympathetic receptors (including those cells that have receptors but do not receive parasympathetic innervation, such as some blood vessels).

Answer 47

Acetylcholine is not a marketed drug because it must be injected and has an extremely short duration of effect. * Two types of drugs are used: derivatives of acetylcholine carbachol, bethanechol [Urecholine] * and cholinomimetic alkaloids (pilocarpine).

Answer 48

•Eyes: Decrease intraocular pressure in glaucoma, miosis

Answer 49

•Resp: Stimulates secretions in the tracheobronchial tree, produces bronchoconstriction

Answer 50

•Cardiovascular: Decrease in heart rate and force of contractility is due to cholinergic innervation of the SA and AV nodes and atrial muscle.

Answer 51

•GI: Increased tone and amplitude of contraction, peristaltic activity, and secretory action.

Answer 52

•Urinary tract: Increase in ureteral peristalsis and contraction of the detrusor muscle.

Answer 53

•Neuromuscular: Treat Myasthenia gravis, Reverse neuromuscular block

Answer 54

* GI discomfort: nausea, vomiting, diarrhea, belching, salivation, and intestinal cramps * Bradycardia * Bronchoconstriction

Answer 55

MOA: * Increases tone of detrusor muscle and causes bladder contractions * Increases tone of the lower esophageal sphincter

Answer 56

Urinary retention (Post-op & post-partum)

Answer 57

Initially: * Abdominal discomfort/ epigastric pain, salivation, flushed skin, sweating, nausea, vomiting, and miosis are common. Toxic reactions: * include intense cramping, diarrhea, urination, bradycardia, and bronchoconstriction.

Answer 58

COPD, asthma, hyperthyroidism, peptic ulcer

Answer 59

Education: To avoid nausea & vomiting, take 1 hour before or 2 hours after meals.

Answer 60

* **_Used primarily as an ophthalmic solution in the treatment of open-angle glaucoma_** where, by contracting the ciliary muscle, outflow of aqueous humor is improved and intraocular pressure reduced within minutes. * **_Used also to treat of xerostomia and Sjogren ’s syndrome because it increases salivation_**.

Answer 61

•Prototype: neostigmine bromide (Prostigmin); Also use pyridostigmine (Regonol)

Answer 62

* These drugs produce reversible inhibition of AChE (which destroys Ach) * by formation of a carbamyl-ester complex which dissociates slowly, * hence provides longer action of Ach. * They act preferentially at the neuromuscular junction (NMJ) and * restore skeletal muscle strength by increasing the availability of acetylcholine.

Answer 63

**_Myasthenia gravis_** and Nondepol Neuromuscular Blockade Reversal

Answer 64

•nausea, diarrhea, and excessive salivation. **Caution in patients with asthma.** If muscarinic effects of such therapy are prominent, they can be controlled by the administration of atropine.

Answer 65

Note that there is a short amount of time between the occurrence of ADRs and Toxicity- **_emergency treatment needed if you see fasciculations of voluntary muscles_**.

Answer 66

•Donepezil (Aricept)

Answer 67

•inhibits breakdown of AChE; thus causing an increase in Ach (Donepezil (Aricept))

Answer 68

Treatment of mild to moderate Alzheimer's disease. Among those who benefit, improvements are seen in quality of life and cognitive functions (eg, memory, thought, reasoning). There is no evidence the drug leads to substantial functional improvement or prevents progression of Alzheimer’s.

Answer 69

Most ADRs are related to increased cholinergic (muscarinic) effects including GI effects such as nausea and diarrhea, increases gastric acid secretion (monitor for occult bleeding), syncope, bradycardia (thus should be taken at bedtime)

Answer 70

Patients with Alzheimer disease (AD) have reduced cerebral production of choline acetyl transferase, which leads to a decrease in acetylcholine synthesis and impaired cortical cholinergic function.

Answer 71

Donepazil has an advantage over other drugs such as tacrine (another centrally active AchE inhibitor that was the first drug to show success treating AD) because of **once-a day** **dosing** (improved adherence), **lower side effect profile**, and **does not require liver function tests for hepatoxicity.**

Answer 72

cholinergic blockers, muscarinic antagonists

Answer 73

MOA: Block Ach at muscarinic receptors Prototype: atropine

Answer 74

To get mydriasis

Answer 75

* Blocks vagal impulses to heart * Reverses sinus brady (increases HR)

Answer 76

* Bronchodilation * SuprprSuppressratory secretions pre-op

Answer 77

Decreases secretions and tone.

Answer 78

to treat bladder spasms

Answer 79

* Treat tremors/rigidity of Parkinsonism * Treat EPS from psychotropic medications * Sedation * Motion Sickness

Answer 80

* Photophobia * Increased Intraocular Pressure * Dry Mouth * Constipation * Urinary retention * Drowsiness * Central Anticholinergic Syndrome/ Anticholinergic toxicity (antidote is physostigmine salicylate- increases Ach)

Answer 81

Atropine or scopolamine is administered prior to induction of anesthesia to **_protect_** **_heart_** **_from vagal reflexes and prevent excessive salivary & respiratory secretions_**. Pts. w/ glucome requires special consideration

Answer 82

•Atropine is used to reverse severe sinus bradycardia in adults and neonates, especially when due to parasympathetic influence (e.g., digoxin, beta blockers).

Answer 83

•Atropine decreases the tone of the smooth muscle of the biliary tract & ureter and produce relaxation.

Answer 84

Motion Sickness Prevention: Protection is greatest if the scopolamine is applied as a patch [Transderm-Scop] behind the ear at least four hours before the noxious stimulus.

Answer 85

Anticholinergic drugs can relax bronchial smooth muscles by blocking the constrictor effects of the vagus nerve. The anticholinergic drugs are more effective bronchodilators when administered by aerosol inhalation

Answer 86

In spite of their bronchodilatory effect, systemic anticholinergics should be used cautiously in asthmatic patients because of drying of secretions and increased risk of mucus plugs.

Answer 87

**_Anticholinergics_** are recommended as a first line drug be used in treating COPD

Answer 88

•is the prototype of overactive bladder drugs. Oxybutynin is both an antimuscarinic and an antispasmodic. It easily crosses the blood-brain barrier, thus has a higher rate of CNS adverse effects. inform the patient that adverse effects include xerostomia (70%) constipation, urinary retention, and blurred vision. Alcohol may enhance the drowsiness

Answer 89

Anticholinergic drug - •commonly advertised drug for overactive bladder.

Answer 90

Anticholinergic adverse effects (dry mouth, blurred vision, constipation, cognitive dysfunction). This is challenging because the population with the highest prevalence of overactive bladder is the elderly: patients predisposed to cognitive dysfunction, urinary retention and visual disturbances.

Answer 91

* Parkinson’s Disease & extrapyramidal symptoms of antipsychotics. * Parkinsonian tremor and rigidity seem to result from a relative excess of cholinergic activity in the basal ganglia system. * The tremor of Parkinson’s disease is reduced by centrally acting antimuscarinic drugs * (e.g., benztropine [Cogentin]; trihexyphenidyl [Artane]).

Answer 92

Is often recommended to alleviate extrapyramidal symptoms (EPS) associated with conventional antipsychotic agents.

Answer 93

**Nondepolarizing Agents** _Tubocurarine_ is the prototype drug but is no longer available in the US **Depolarizing Agents** _Succinylcholine_ [Anectine] (two acetylcholine molecules attached) is the only agent.

Answer 94

To be clear, an anticholinergic drug is NOT an adrenergic agonist (their pre-ganglionic mechanism of action and post-ganglionic transmitters vary). But their EFFECT is similar and that might help for you to remember their uses and side effects.

Drugs affecting Autonomic Nervous System Flashcards

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