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811 > Drugs in Red - Exam 3 > Flashcards

Drugs in Red - Exam 3 Flashcards

1
Q

Muscarine

A
  • Cholinergic drug that mimics ACh actions on ACh muscarinic receptors
  • Elicits parasympathetic response generally speaking
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2
Q

Atropine

A
  • Anticholinergic drug
  • Prototype Muscarinic Receptor Antagonist (Blocker)
  • Tertiary amine
  • One of the active compounds of Belladonna (d,l-hyoscyamine)
  • Increases heart rate, may cause tachycardia
  • Used in organophosphate poisoning to clear chest secretions and increase heart rate
  • Clinical doses have little CNS actions
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3
Q

Varenicline Tartrate

A
  • Chantix
  • Partial CNS nicotinic receptor agonist
  • Stimulates Alpha4/Beta2 nicotinic AChR
  • Relieves cravings and withdrawal symptoms
  • Greater affinity than nicotine, so acts as an antagonist towards nicotine delivery and reduces the reward of smoking
  • SE: Nausea, sleep disturbances
  • FDA Warning: can worse neuropsychiatric symptoms like depression, agitation, and suicidal thoughts
  • Pregnancy Category C
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4
Q

Nicotinic Muscle Receptor Antagonists (4)

A
  • Tubocurarine
  • Pancuronium
  • Atracurium
  • Vecuronium
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5
Q

Nicotinic Ganglionic Receptor Antagonist

A

Mecamylamine

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6
Q

Nicotinic CNS Receptor Agonist

A

Chantix (Varenicline)

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7
Q

Donepexil

A
  • Inhibitor of AChE
  • Used to treat Alzheimer’s
  • Increases ACh in brain
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8
Q

Muscarinic Receptor Antagonists (Not Subtype Specific)

A
  • Atropine
  • Ipratropium
  • Tiotropium
  • Dicycloverine
  • Oxybutynin
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9
Q

Propranolol/Esmolol

A
  • Beta 1 Antagonists
  • Slows heart rate
  • May cause bradycardia
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10
Q

Sildenafil, Tadalafil, Vardenafil

A
  • Viagra, Cialis, and Levitra
  • PDE5 Inhibitors
  • Inhibits breakdown of cGMP
  • Prolongs cGMP’s effect: vasodilation
  • Longer erections
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11
Q

Acetylcholine (Ophthalmic)

A
  • Miochol-E
  • Used in glaucoma or cataract surgery
  • Miosis of iris which increases outflow of aqueous humor
  • Quickly broken down by AChE, systemic responses rare
  • Rare side effects: bradycardia, hypotension, flushing, breathing difficulties and sweating
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12
Q

Pilocarpine (Ophthalmic)

A
  • Isopto Carpine
  • Reduces IOP by facilitating humor outflow
  • Contracts ciliary muscle and iris sphincter (miosis) which opens trabechular meshwork and angle narrowing
  • Less resistance to outflow, less IOP
  • Can cause headache, issues with vision, eye pain
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13
Q

Isopto Carpine Therapeutic Uses (3)

A

1) Reduces elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension.
2) Prevention of Postoperative Elevated IOP associated
with laser surgery.
3) Induction of Miosis

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14
Q

Carbachol

A
  • Miostat
  • Contracts iris sphincter and ciliary body
  • Relieves increased IOP for first 24 hours after cataract surgery
  • Systemic SE: flushing, sweating, epigastric distress, abdominal cramps, tightness in urinary bladder.
  • Use caution with patients with acute cardiac failure, bronchial asthma, GI spasm, or urinary bladder obstruction
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15
Q

Timolol

A
  • Betimol, Timoptic
  • Beta Adrenergic Antagonist, alternate glaucoma therapy
  • Decreases aqueous humor production by ciliary bodies
  • Beta 1 and 2 antagonists (non-selective)
  • Reduces IOP in glaucoma and normal patients
  • SE: worsening asthma, emphysema, bradycardia
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16
Q

Betaxolol

A
  • Betoptic
  • Beta-adrenergic antagonist, alternative therapy for glaucoma
  • Beta-1 antagonist (selective)
  • Decreases aqueous humor production by ciliary bodies
  • Less cardiac/pulmonary effects than Timolol
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17
Q

Pilocarpine (Oral)

A
  • Salagen
  • Tablets for dry mouth from salivary gland hypofunction
  • Radiotherapy or Sjogren’s syndrome can cause this
  • Main side effect: sweating
  • Use caution with patients with CV disease or COPY, asthma, or bronchitis
  • Prolonged muscarinic activation in those with pseudocholinesterase genetic alterations
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18
Q

Cevimeline

A
  • Evoxac
  • Capsule, TID
  • Treats dry mouth for Sjogren’s Syndrome
  • Chol. muscarinic receptor agonist that increases exocrine gland secretions (saliva, sweat) and increases tone to GI/urinary tract
  • Main side effect: excessive sweating
  • Use caution in those with CV disease or pulmonary disease
  • Use atropine or epinephrine to reverse its effects in emergency situations (overdose, extreme cardiac/respiratory depression)
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19
Q

Mirabegron

A
  • Myrbetriq
  • Beta 3 agonist
  • Relaxes bladder
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20
Q

Bethanechol

A
  • Duvoid, Urecholine
  • Muscarinic agonist
  • Increases urinary muscle tone to produce contraction and empty bladder
  • Increases GI muscle tone to restore impair peristalsis
  • Used in non-obstructive urinary retention, neurogenic atony of nerves to bladder
  • Main side effects: cholinergic digestive effects
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21
Q

Bethanechol Precaution

A

If sphincter doesn’t relax when the drug contracts the bladder, urine may be forced up ureter into the renal pelvis and could cause reflux infections.

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22
Q

Succinylcholine

A
  • Depolarizing NM Blocker
  • Skeletal muscle relaxant
  • Phase I: depolarizes skeletal muscle and produces fasciculations (SE: Sore muscles)
  • Phase II: constant stimulation of receptor inactivates it and causes flaccid paralysis
  • AChE inhibitors may augment the effect
  • Sleep apnea reaching up to 60-120 minutes in those with pseudocholinesterase genetic variations
  • Action is terminated when it diffuses form synapse to blood stream
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23
Q

Cocaine

A
  • Local anesthetics
  • Usually 30-50% of injected cocaine is metabolized by pseudo. ChE rapidly
  • If a genetic variation or hepatic disease is present and these enzyme levels are lowered, users will have increases sensitivity to small doses and could have a greater risk of toxicity and death
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24
Q

Edrophonium

A
  • Enlon
  • AntiChE, short acting
  • Quat. ammonium compound
  • Binds to anionic site only, no covalent bond
  • Reversible and brief action
  • Used to diagnose myasthenia gravis, treat a myasthenia gravis crisis in an emergency, or reverse a NM blockage produced by non-depolarizing blockers
  • Side effects similar to direct Ch agonists
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25
Q

Neostigmine

A
  • Prostigmine
  • AntiChE, intermediate duration
  • Quat. ammonium
  • Contains carbamyl ester
  • Increases gastric contractions and secretions, increases sphincter tone and peristalsis in esophagus, increases motility in intestines in those with ileus
  • Direct effect on skeletal muscle and produces contraction
  • Could potentially be used to reverse competitive neuromuscular blocking agents and in treating myasthenia gravis
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26
Q

Pyridostigmine

A
  • Mestinon, Regonol
  • AntiChE, intermediate duration
  • Quat. ammonium
  • Contains carbamyl ester
  • May have direct effect on NMJ
  • Could potentially be used to reverse competitive neuromuscular blocking agents and in treating myasthenia gravis
  • FDA approved for prophylaxis against soman, an organophosphate
  • Clinical effect: 10-15 minutes
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27
Q

Echothiophate

A
  • Phospholine
  • Irreversible AntiChE
  • Contains a liable leaving group like fluoride or parathion
  • No spontaneous hydrolysis can occur and enzyme is inactivated
  • Used to treat glaucoma by contracting ciliary muscle and pupil sphincter (miosis)
  • Reserved for those not responding or tolerating other therapy due to systemic effects
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28
Q

Benzodiazepines

A
  • Used IV in organophosphate poisoning

- Treats agitation and seizures

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29
Q

Oximes

A
  • 2-PAM
  • Infused
  • Need to use early to reverse organophosphate binding before aging can take place
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30
Q

Edrophonium Drug Interactions

A
  1. Other AChE compounds - potentiation of effects can cause a cholinergic crisis.
  2. NMJ blocker Succinylcholine- may prolong block.
  3. Digitalis, Pilocarpine - additive, slows heart
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31
Q

Edrophonium Contraindication

A
  • Asmathetics

- Urinary or intestinal obstructions

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32
Q

Neostigmine Side Effects

A
  1. Exaggerated pharmacological effects like fasciulation and salivation
  2. Bowel cramps and diarrhea may also occur
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33
Q

Neostigmine Methylsulfate

A
  • IM or SC
  • Myasthenia gravis symptom control when oral isn’t an option
  • Prevents urinary retention and distention after surgery
  • Reverses non-depolarizing NM blocking agents after surgery
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34
Q

Pyridostigmine Side Effects

A
  • Standard doses - fasciculations
  • High doses - muscle weakness
  • Abdominal cramps and diarrhea
  • Used IV in hospital emergencies, may cause bronchial secretions and arrhythmias
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35
Q

Physostigmine

A
  • Eserine
  • AntiChE, intermediate duration
  • Contains a carbamyl ester
  • Used to treat anticholinergic drug toxicity, reverse muscarinic blockades, in glaucoma
  • Crosses BBB, may cause seizures
  • Increased duration in those when pseudo. ChE variations or hepatic disease
  • Similar side effects to edrophonium, increases duration and potency can make them more severe though
  • Don’t use in those with asthma, CV disease, or urinary/intestinal block
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36
Q

Corticosteroids + Myasthenia Gravis

A
  • Prednisone
  • Clinical effect time: 2-8 weeks
  • Decreases AChR antibody levels
  • Alternate dosing days
  • Side effects: weight gain, decreased bone density, GI irritation
37
Q

Oral Immunosuppressant Medications + Myasthenia Gravis

A
  • Cyclosporine - clinical effect time of 2-6 months
  • Azathioprine - clinical effect time of 3-18 months
  • Inhibit T and B lymphocytes and IL-2
38
Q

Donepezil

A
  • Aricept
  • Cholinesterase inhibitor approved to treat mild to moderate Alzheimers
  • Drug do not reverse Alzheimers, just slow the progression
  • Side effects: cholinergic (N/V, diarrhea, bradycardia)
39
Q

Rivastigmine

A
  • Exelon
  • Cholinesterase inhibitor approved to treat mild-moderate Alzheimers
  • Available as a patch, may have less N/V and more CNS selectivity
  • Drug do not reverse Alzheimers, just slow the progression
  • Side effects: cholinergic (N/V, diarrhea, bradycardia)
40
Q

Memantine

A
  • Namenda
  • NMDA Receptor antagonist
  • Prevent/slow rate of memory loss in Vascular-dementia and Alzheimers (even in moderate to severe patients)
  • Few drug-drug interactions and adverse events
  • Side effects: confusion, agitation, restlessness
  • High doses produce ketamine or PCP-like effects (hallucinations, stupor)
41
Q

Scopolamine

A
  • Hyoscine
  • Active compound in Belladonna with anticholinergic properties
  • Clinical doses cause CNS depression with drowsiness, amnesia, and fatigue
  • Patch
  • Used for motion sickness and to recover from anesthesia and surgery
  • Side effects: Dry mouth and drowsiness
  • May worse open-angle glaucoma from mydriatic effect
42
Q

Antimuscarinic Agents (5)

A
  • Atropine
  • Ipratropium
  • Scopolamine
  • Cyclopentolate
  • Tropicamide
43
Q

Long-Acting Antimuscarinic Agents (2)

A
  • Tiotropium

- Aclindium

44
Q

Atropine Dose-Based Side Effects

A
  1. Low doses: depress salivary/bronchial secretions & sweating.
  2. Moderate doses: pupil dilates, accommodation of the lens to near vision is inhibited, and heart rate is increased.
  3. Larger doses: antagonize ACH control of the urinary bladder and gastrointestinal tract, thereby inhibiting micturition and reducing the tone and motility of the gut (constipation)
  4. Highest dose: greater inhibition - gastric motility/secretion.
45
Q

Benztropine

A
  • Cogentin
  • Helps correct imbalance of dopamine and ACh in CNS
  • Used to treat Parkinsons and post-antipsychotic treatment
  • SE: confusion, memory problems, anticholinergic in PNS
46
Q

Trihexyphenidyl

A
  • Artane
  • Helps correct imbalance of dopamine and ACh in CNS
  • Used to treat Parkinsons and post-antipsychotic treatment
  • SE: confusion, memory problems, anticholinergic in PNS
47
Q

Tropicamide

A
  • Mydriacyl
  • Dilates pupil, paralyzes ciliary muscle, abolishes normal pupil reflex to light
  • Used to examine retina and optic disc, used to reduce painful ciliary muscle spasm
  • Side effects: photophobia, transient stinging and rise in IOP, acute attacks of angle-closure glaucoma in rare cases
48
Q

Atropen

A

-Abboject, Atropine auto-injector
-Abolishes vagal reflex to slow heart or asystole from pressure on eyeball, peritoneal stimulation, or injection of contrast dye in cardiac catheterization
-Mainly used in ICU and in short-term interventions
-Also can increase heart rate or decrease AV-block from excess vagal tone
SE: counteracts systemic ACh agonists’ effects like BP drops and vasodilation, no effect when given alone from lack of cholinergic innervation in blood vessels

49
Q

Ipratropium

A
  • Atrovent
  • Short acting anticholinergic
  • Inhalation
  • Used to treat asthma and COPD
  • Relieves rhinorrhea from cold and allergic rhinitis
  • DOESN’T relieve nasal congestion or sneezing
  • Causes bronchodilation
  • Minimally absorbed systemically due to quat. ammonium
  • Not selective between muscarinic receptors, dissociates a little more slowely from M3 than M2 making its duration ~3-4 hours
50
Q

Tiotropium

A
  • Spiriva
  • Long acting anticholinergic and bronchodilator
  • Inhalation
  • Used to treat moderate to very severe COPD
  • Quat. ammonium with low systemic absorption and no CNS effects
  • Dissociates MUCH slower from M3 receptor making it more selective and prolonged in activity, duration ~24 hours or more
51
Q

Belladonna & Opium

A
  • Suppositories
  • Include morphine, atropine, and scopolamine
  • Used to treat severe pain from uretal spasms or rectal/bladder tenesmus in post-op or neoplastic states
52
Q

Donnatal Extentabs

A
  • FDA: “possibly effective”
  • Contains antimuscarinics
  • Adjunctive therapy in IBS and duodenal ulcers
  • Could cause urinary retention, tachycardia, mydriasis, xerostomia, and constipation
53
Q

Dicyclomine

A
  • Bentyl
  • Treats functional bowel disorder and IBS
  • Relieves smooth muscle spasms by having an antimuscarinic effect and directly acting on smooth muscle by antagonizing bradykinin and histamine caused spasms
  • Side effects: anticholinergic
54
Q

Oxybutynin

A
  • Ditropan
  • Treats overactive bladder
  • Muscarinic antagonist
  • Decrease the normal tone and amplitudes of contractions in the ureter and bladder
  • Available in many forms, gel, syrup, tablets, patch
  • Patch may produce fewer anticholinergic effects
55
Q

Tolterodine

A
  • Detrol
  • Treats overactive bladder
  • Muscarinic antagonist
  • Decrease the normal tone and amplitudes of contractions in the ureter and bladder
  • Tablets
56
Q

Overactive Bladder Drug Precautions

A
  • Caution when treating patients with urinary or gastric retention
  • Caution in patient with decreased GI motility
57
Q

Hydrocodone

A
  • Analgesic
  • Relief of cough, nasal congestion, and moderate pain
  • High abuse potential
58
Q

-Hycodan

A
  • Hydrocodone + Homatropine
  • Tablet or liquid form
  • Homatropine is an anticholinergic that discourages abuse of the product
59
Q

Diphenoxylate

A
  • Lomotil
  • Schedule V
  • Prescribed orally to treat diarrhea
  • Diphenoxylate + Atropine to discourage abuse
60
Q

Albuterol

A
  • B2 selective agonist
  • Dilates bronchi
  • Used to treat mild to very severe COPD
  • If absorbed, little effect on B1 cardiac receptors since it is selective
  • Short acting
  • Inhalation
61
Q

Combivent/Duoneb

A
  • Combinations of Albuterol and Ipratropium
  • Caution using with other anticholinergic drugs and in those with CV disorders
  • Inhalation
62
Q

Salmeterol

A
  • Severent Diskus
  • B2 selective agonists
  • Long-acting bronchodilator
  • Used to treat moderate to very severe COPD
  • Inhalation
63
Q

Combination LABA/LAAC

A
  • Vilanterol/Umeclindium (Anoro Ellipta)
  • Olodaterol/Tiotropium (Stiolto Respimat)
  • Inhalation
  • Once daily
  • Used to treat moderate to very severe COPD
64
Q

Fluticasone

A
  • Flovent
  • Inhaled anti-inflammatory drug
  • Used to treat severe to very severe COPD
  • Mometasone and Fluticasone have <1% systemic absorption (act locally in lung)
65
Q

Fluticasone + Salmeterol

A
  • Advair HFA
  • Inhaled anti-inflammatory + B2 agonist
  • Used to treat severe to very severe COPD
66
Q

Theophylline

A
  • Theolair, Slo-phyllin
  • Adenosine receptor antagonist
  • Adenosine constricts the bronchi
  • Used in severe to very severe COPD patients who need additional symptom control
67
Q

CYP3A4 Inhibitors

A
  • Ketconazole
  • Itraconazole
  • Ritonavir
  • Increase the systemic toxicity of inhaled corticosteroids when co-administered
68
Q

CYP3A4 Inducers

A
  • Phenytoin
  • Carbamazepine
  • Phenobarbital
  • Rifampin
  • No change in toxicity when co-administered with inhaled corticosteroids (since systemic absorption is already so small)
69
Q

Roflumilast

A
  • Daliresp
  • Selective PDE4 inhibitor, cAMP metabolizing enzyme in the lung
  • Reduces risk of COPD exacerbations in severe COPD
  • Not a bronchodilator or indicated for relief of bronchospasms
  • Main side effects: diarrhea, weight loss, nausea, psychiatric adverse reactions
70
Q

Nicotine

A
  • Acts on both sympathetic and parasympathetic ganglia
  • Increases blood pressure from sympathetic activation (releases epi. from adrenal glands and norepi. on blood vessels not innervated by parasymp.)
  • Increases GI/urinary tract peristalsis and secretions from parasympathetic activation
  • Activates activity that predominates the associated organ system
  • Tertiary amine with no therapeutic benefits
  • Highly lipid soluble and can enter CNS
  • Releases dopamine and opiate peptides onto nucleus accumbens to create dependence and cravings
  • Withdrawal occurs within 24 hours after quitting
71
Q

Mecamylamine

A
  • Inversine
  • Reduces blood pressure in normal and hypertensive patients
  • Noncompetitive antagonist of nicotinic AChR in ganglia
  • Uses in those with essential hypertension and malignant hypertension
  • D/C slowly since sudden stopping could cause strokes or heart failures
72
Q

Mecamylamine Side Effects

A
  1. GI: Ileus, constipation, dry mouth
  2. CV: hypotension, dizziness, mild tachycardia
  3. NS/Psychiatric: convulsions, tremors, sedation
  4. Urogenital: urinary retention
73
Q

Tubocurarine

A
  • Non-depolarizing NM Blocker prototype

- Replaced with other drugs due to SE including histamine release and hypotension

74
Q

Cisatracurium

A
  • Nimbex
  • Degrades in plasma spontaneously
  • Non-depolarizing NM Blocker
  • Good to use in those with renal failure
75
Q

Pancuronium

A
  • Pavulon
  • Non-depolarizing NM Blocker
  • Increases heart rate
  • Don’t use in kidney disease patients
76
Q

Rocuronium

A
  • Zemuron
  • Non-depolarizing NM Blocker
  • Rapid onset
  • Used for tracheal intubation
  • Don’t use in liver disease patients
77
Q

Vecuronium

A
  • Norcuron
  • Non-depolarizing NM Blocker
  • Used for mechanical ventilation in ICU
  • Also reduces oxygen consumption, protects surgical wounds/medical device placement, helps control elevated intracranial pressures, prevents muscle spasms
  • Don’t use in patients with liver disease
78
Q

Suggammadex

A
  • Bridion
  • Reversal of rocuronium and vecuronium induced NM blockade
  • Renally excreted unchanged, don’t use in renally impaired patients
  • Adverse effects: N/V, hypotension, pain, and headache
  • Forms a complex with NM blocker to reduce the amount available to block NM receptors
79
Q

Succinylcholine Uses

A
  1. Facilitate tracheal intubation
  2. Adjunct to general anesthesia
  3. Skeletal muscle relaxation during surgery or mechanical ventilation
  4. Electroconvulsaive Shock Therapy (ECT)
80
Q

Succinylcholine Black Box

A

Those with undiagnosed skeletal muscle myopathy (usually Duchenne’s muscular dystrophy) who are administered succinylcholine may experience acute rhabdomyolysis with hyperkalemia. This will progress to cardiac arrest and death.

81
Q

Cotinine

A
  • Best biomarker for nicotine use
  • Half life is about 16-20 hours
  • Can be measured in urine, serum, saliva, and hair
82
Q

Transdermal Nicotine Patches

A
  • Slowest delivery to CNS
  • 6-8 hours to reach peak
  • Start before quitting smoking
  • Can cause pruritus, insomnia, and vivid dreams
  • Remove before bed to avoid sleeping disturbances
  • Try different brands if pruritus arises
  • Pregnancy Category D
83
Q

Nicotine Oral Replacement

A
  • Absorbed through oral mucosa
  • Gum, lozenges, oral inhalers
  • Peak reached in 20-60 minutes
  • Highly susceptible to first pass metabolism if swallowed
  • Causes nausea and indigestion if swallowed
  • Pregnancy Category D
84
Q

Nicotine Nasal Spray

A
  • Fastest onset: 5-20 minutes
  • Doubled cessation rates when used with patch
  • May cause transient burning and stinging, throat irritation, rhinorrhea, and nausea
  • Pregnancy Category D
85
Q

Bupropion SR

A
  • Catecholamine reuptake inhibitor

- Used to treat depression

86
Q

Bupropion

A
  • Zyban
  • FDA approved to treat tobacco dependence
  • Increases cessation rates to 36% when used with patch
  • Adverse events: insomnia and dry mouth
  • Don’t take if there is a history of seizure, stroke, or brain tumors/injuries
  • Pregnancy Category C
87
Q

Clonidine

A
  • Catapres
  • Not FDA approved for smoking cessation
  • Used in those who cannot tolerate other nicotine replacement therapies or drugs
  • Inhibits symp. NS activation by CNS
  • Mixed results on whether it is effective in smoking cessation
88
Q

Nortriptyline

A
  • Pamelor
  • TCA
  • Improves cessation rates to 23% when used with patch
89
Q

Rimonabant

A
  • Acomplia
  • Antagonist of cannabinoid type 1 receptors
  • Decreases nicotine self-administration

811 (38 decks)

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