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Pharm 2 Flashcards

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0
Q

Cholinergic agonists

A

Act on ACh sites or with ACh-esterase

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1
Q

Acetylcholinesterase

A

Enzyme that breaks down acetylcholine.

Prevents overstimulation of cholinergic receptor sites

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2
Q

Bethanechol

A

Tx of neurogenic bladder in kids over 8

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3
Q

Children and cholinergic agonists

A

Kids r more at risk for adverse effects. GI upset, diarrhea, increased salivation could cause choking, bowel/bladder control loss,

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4
Q

Tx of myasthenia gravis or reversal of neuromuscular junction blocker effects in kids

A

Neostigmine and pyridostigmine

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5
Q

Parasympathomimetic

A

Mimicking effects of PNS-bradycardia, hypotension, pupil constriction, <bladder tone, relax sphincters, & bronchoconstriction

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6
Q

Myasthenia Gravis

A

Autoimmune disease characterized by antibodies to cholinergic receptor sites. Causes destruction of the receptor sites and decreased response at the neuromuscular junction. Progressive, debilitating, leading to paralysis

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7
Q

Direct-acting cholinergic agonists

A

Are similar to ACh and react directly with receptor sites as if ACh had stimulated it. These drugs usually stimulate muscarinic receptors W/I the PNS. Used as systemic agents to increase bladder tone, urinary excretion, and GI secretions, and as ophthalmic agents to induce mitosis to relieve intraocular pressure if glaucoma. No systemic absorption usually occurs

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8
Q

Indirect-acting cholinergic agonists

A

Cause increased stimulation of the ACh receptor sites by reacting with the enzyme acetylcholinesterase and preventing it from from breaking down the ACh

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9
Q

Direct acting cholinergic drugs

A

Bethanechol (duvoid, urecholine)
Carbachol (miostat)
Cevimeline (evoxac)
Pilocarpine (pilocar)

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10
Q

Cholinergic agonist are usually associated with many undesirable effects

A

Because their action cannot be limited to a specific site their effects are widespread throughout the body
Used infrequently

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11
Q

Endrophonium

A

Is used only to dx myasthenia gravis

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12
Q

Therapeutic effects of direct-acting cholinergic agonists

A

Mimic effects of ACh and parasympathetic stimulation.
Slowed HR, >myocardial contractility, vasodilation, bronchconstriction, <bladder tone, relaxed bladder and GI sphincters, pupil constriction

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13
Q

Uses of Bethanechol=affinity for cholinergic receptors in urinary bladder.
Oral or subQ

A

Tx of nonobstructive postoperative and postpartum urinary retention.
Neurogenic bladder atony in adults and in kids older than 8.
Dx and Tx of reflux esophagitis in adults. And Tx of infant &kids for esophageal reflux

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14
Q

Carbachol

A

Available as ophthalmic agent used to induce miosis or pupil constriction to relieve pressure in glaucoma. Used for some eye surgeries

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15
Q

Cevimelind and pilocarpine which bind to muscarinic receptor throughout the system

A

Used to increase mouth & GI secretions, relieve dry mouth or symptoms of sjogrens

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16
Q

General contraindications of direct cholinergic agonists

A

Undesirable systemic PNS stimulation. Condition exacerbation
CAD-cardiac suppression, bradycardia, hypotension, vasomotor instability, peptic ulcer, GI block or surgery, asthma, bladder surgery, epilepsy, Parkinson’s

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17
Q

Adverse effects of direct cholinergic agonists

A

PNS stimulation- hypoTN, bradycardia, heart block, cardiac arrest. GI: N,V,D cramps, salivation,shart. Swallowing w/ cevimeline and pylocarpine, incont

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18
Q

Drug-drug for direct cholinergic agonists

A

Acetylcholinesterase inhibitors like neostigmine and tacrine. <risk of overstimulation of PNS

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19
Q

Implementation of cholinergic agonist direct acting

A

Proper ophthalmic admin to >risk of systemic absorption.
Oral drugs on empty stomach >GI problems
Monitor & keep cholinergic block like Atropine

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20
Q

Miosis

A

Pupillary constriction

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21
Q

Nerve gas

Unlike most indirect acting cholinergic agonists

A

An indirect acting cholinergic agonist. Irreversibly binds w/acetylcholinesterase. ACh accumulates and death by muscle rigor

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22
Q

Irreversible direct acting cholinergic agonists

A

Not used therapeutically

Antidote for nerve has=pralidoxime and for Tx of poisoning by organophosphate pesticides

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23
Q

Two categories of reversible indirect acting cholinergic agonists

A
  • used to treat myasthenia gravis

* used to treat AD

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24
Q

Myasthenic crisis vs cholinergic crisis

A

Myasthenic crisis=drug

Drug diagnosis=endrpphonium inj

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25
Q

Drugs: Indirect acting cholinergic agonist

MG category

A

Ambenonium (Mytelase)-MG adult
Endrophonium (Reversol)-dx MG crisis rev. paralytic drugs of surgery
Neostigmine (Prostigmin)-Dx & Tx of MG rev. Paralytic drug of surgery
Pyridostigmine (Mestinon)- mgmt of MG. Antidote for nerve gas

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26
Q

Drugs: indirect acting cholinergic agonists

AD category

A

Donepezil (Aricept)-mgmt AD & severe dementia.
Galantamine (razadyne)-mgmt & delays mild/moderate AD dementia.
Rivastigmine (excelon)-mgmt mi/mod AD Tx dementia of Parkinso
Tacrine (cognex)-4 AD yanked 2012

27
Q

Alzheimer’s disease

A

Progressive neural degeneration in cortex=memory loss, >ADL’s,
>ACh producing neurons and their target beurons

28
Q

Memantine

A

Tx AD -blocks various receptor sites in brain slows plaque build-up on axons. Slows/delays AD.

29
Q

Contraindications cautions of indirect acting cholinergic agonists
Anticholinesterase

A

Pregnancy- induce labor

Usually effects r localized to cortex and neuromuscular jxn, however same cautions about Systemic PNS

30
Q

Indications for anticholinergic drugs

A
  • > secretions prior to anesthesia
  • Tx Parkinson’s by block ACh stim
  • restor HR & BP post surgical vagal stim.
  • Tx bradycardia from carotid sinus reflex hyperactivity
  • Tx pylorospasm and hyper bowel
  • Tx motion sickness
  • relax biliary and ureteral colic
  • relax blad detrusors/tightsphincters
  • control lagh cry in brain injury
  • relax uterine hypertonicity
  • mgmt of peptic ulcer
  • control rhinorhea hay fever
  • antidote for cholinergics/mushroom
  • ophthalmic mydriasis/cycloplegia
31
Q

Mydriasis

A

Relaxation of the pupil

32
Q

Cycloplegia

A

Inhibition of lens to accommodate near vision

33
Q

Fx of atropine and scopolamine

A

Work by blocking only muscarinic effectors in the PsNS and a few cholinergic receptors in SNS. Those that <sweating. Compete with ACh do not block nicotinic

34
Q

Flavoxate any trospium

A

Act specifically on smoot muscle of urinary tract. Tx overactive bladder and bladder spasms.

35
Q

Ipratropium and tiotropium

A

Act specifically to >respiratory secretions and cause bronchodilation

36
Q

Cyclizine and meclizine

A

Reduce sensitivity of labarynth apparatus
•partially bloc cholinergic chemoreceptor trigger zone
>motion sickness prevent N,V

37
Q

Hyoscyamine and methscopolomine

A

Act specifically on receptor in GI tract. Tx peptic ulcer, IBS, GI disorders

38
Q

Antichoinergics and kids

A

Used often in kIds, but kids more sensitive to adverse effects constipation, urinary retention, heat int., confusion.
Dycyclomine not for kids!

39
Q

Anticholinergics in older adults

A

Extreme caution. Adverse effects increased. Heat intolerance. Confusion, hallucination, psychotic syndromes. Renal imp. Lower dose

40
Q

African Americans mydriatic effects

A

Increased dose for dark pigmented eye to achieve mydriatic effect

41
Q

Anticholinergics contraindicated in conditions that could exacerbate

A

Glaucoma-poss. Increase in intraocular pressure
Stenosing peptic ulcer, intestinal atony, paralytic ileus, GI block, severe ulcerative colitis, toxic megacolon, prostatic hypertrophy, bladder block, cardiac arrhythmia, tachycardia, myocardial ischemia, kidney/liver imp., MG-low dos sometimes used.

42
Q

Adverse effects of anticholinergics

A

Systemic blocking of cholinergic receptors. Adverse effect in one case may be the desired effect I another. Systemic effects dose dependent. CNS effect: blurred vision, pupil dilation, cycloplegia , intraocular pressure. Weaknesses dizziness, insomnia, mental confusion

43
Q

Atropine toxicity

A

Poison belladonna, in a variety of other natural products.
Sudden onset of bizarre mental and neurological symptoms.
10.0mg=coma, dillusion, hallucination. Physostigmine antidote.

44
Q

Drug to drug interactions with antichinergics

A

Antihistamines, antiparkinsonism’s, MAO inhibitors, &tricyclic antidepressants. Phenothiazines effectiveness decreases and <risk of paralytic ileus

45
Q

Monitor patients on antichinergics for

A

Dry mouth, swallowing, constipation, urinary retention, tachycardia, pupil dilation, photophobia, cycloplegia, blurring of vision, heat intolerance >sweatig

46
Q

Propantheline

A

Adjunct in Tx of ulcers

47
Q

Ipratropium

A

Tx COPD, asthma

48
Q

Tiotropium

A

COPD

49
Q

Scopolamine patch

A

Tx N, V, Of motion sickness

Caution for pregnant or lactation

50
Q

Safety of scopolomine patch

A 
Apply to clean/ dry
Wear gloves don't touch adhesive
Change 3 days
Elderly more sensitive 
Remove for defib/CPR or MRI
51
Q

Parkinson’s Disease

A

Loss of dopamine in the substantial nigra of brain

Anticholinergic drugs counter balance the excessive cholinergic activity. Benztropine and diphenhydramine

52
Q

The don’t mix insulins

A

Insulin glargine (Lantus) and insulins detemir ( levemir) cannot be mixed in syringe with anything else

53
Q

Pregnancy/lactation considerations of insulin

A

Doesn’t cross placenta. Can inhibit good nutrient rich breast milk

54
Q

Drug to drug interactions w/insulin

A

MAO inhibitors, beta blockers, salicylates and alcohol decrease glucose levels.
•beta blockers block SNS which hinders ability so see signs of hypoglycemia

55
Q

Herbal remedy and antidiabetics

A

Juniper berry, ginseng, garlic, fenugreek, coriander, dandelion root, celery. = hypoglycemia

56
Q

Sulfonylureas

A

1st oral agents for type 2 DM.
Stimulate pancreas release insulin
Bind to K+ channel on pancreatic beta cells. May improve insulin binding. <effects of anti diuretic hormone on renal cells. Only work if pt. has Fx beta cells. 1st or 2nd gen

57
Q

1st generation sulfonylureas

* may be thought to <CVD and death

A

Chlorpropamide (diabinese) most frequent. Reliable predictable effect
Tolazamide (tolinase) less predictabl
Tolbutamide (Orinase) preferred for pt. w/renal imp. Easily cleared.

58
Q

Sexing generation sulfonylureas

A

Glimepiride (amaryl)-less$$$
Glipizide (Glucotrol)
Glyburide (diabeta & micranase, glynase, prestab)

59
Q

2nd gen sulfonylureas

A

Adjunct to diet/and/or insulin mgmt of type 2
Excreted urine &bile sfr renal imp
Less interaction w/ pro- bound drug
Long acting

60
Q

Severe hypoglycemia

A

<40mg/dL

61
Q

Short acting insulin

A

Humalog, novalog, regular
<15 mins. H &N
30-60min

62
Q

Combo insulin

A

30-60 min

Then 1-2 hour

63
Q

Intermediate insulin

A

NPH and Lente

60-120

64
Q

Long insulin

A

PZ1, Lantus, Ultralente

4-8 hours

65
Q

Short/rapid insulin

A

Aspart, lispro, glusiline (novolog, humalog, apidra)
Onset: 10-20, 15, 20-30
Lasts: 3.5, 3.5-4.5, <6

66
Q

Long acting insulin

A

Glargine (lantus)- 60min, 24+
Detemir (levemir)-60-120min, 24+
Do not mix

Nursing (7 decks)

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