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Flashcards in Bolded Drugs Deck (70):
1

Lidocaine

Local anesthetic - amide
Indx: local anesthesia, neuropathic pain
Mech: block V-gate Na channels in nerve
AE: CNS effects, CV depression, hypersensitivity rxn, hematological effects (methemoglobinemia)
Other: metabolized by liver

2

Benzodiazepine

Spasmolytic agent
Indx: Spasticity due to cerebral palsy, MS, spinal cord injury, stroke, etc.; essential tremor; CINV, PONV; anxiety (panic disorder, GAD); seizures
Mech: Bind to GABAa receptors, increase GABA-mediated IPSP
AE: Sedation, motor impairment, amnesia, tolerance, physical dependence (schedule IV)
Other: Also can be used for acute msc spasm; especially effective in ET aggravated by anxiety; rapid onset of anxiolytic effects
Seizure indx: status epilepticus or, sometimes, absence, atonic, and myoclonic

3

Baclofen

Spasmolytic agent
Indx: Spasticity due to cerebral palsy, MS, spinal cord injury, stroke, etc.
Mech: Agonist GABAb receptors, decrease exocytosis of excitatory NTs (presynaptic), also postsynaptic inhib effect
AE: SKM weakness, dizziness, drowsiness, depression, fatigue @ high doses

4

Tizanidine

Spasmolytic agent
Indx: Spasticity due to cerebral palsy, MS, spinal cord injury, stroke, etc.
Mech: Agonist at a2 receptors, decrease exocytosis of excitatory NTs in brain/spinal cord (presynaptic), also postsyn inhib effect
AE: SKM weakness (less than baclofen), a2 agonist side effects [hypotension, drowsiness, dry mouth]

5

Cyclobenzaprine

Muscle relaxant
Indx: Acute muscle spasm due to local tissue injury, muscle sprains, etc.
Mech: Central effect, probably at brain stem; sedative effects (mech unsure)
AE: Drowsiness, mAChR antag side effects [dry mouth, urinary retention, confusion, attacks of angle-closure glaucoma]

6

Levodopa

DA precursor
Indx: PD, dystonia
Mech: converted to DA by dopaminergic neurons in striatum
AE: n/v, postural hypotension, dyskinesia, confusion
Other: can be administered with carbidopa and/or entacapone to increase bioavailability past BBB

7

Carbidopa

DA precursor
Indx: PD, dystonia
Mech: amino acid dexcarboxylase inhibitor, blocks peripheral conversion of levodopa to DA
AE: n/v (decreases levodopa's effects), postural hypotension, dyskinesia

8

Entacapone

COMT inhibitor
Indx: PD, dystonia
Mech: inhibits DA conversion in the periphery by COM
AE: dyskinesia, nausea, confusion
Other: assists with levodopa bio availability across BBB

9

Ropinirole

DA agonist
Indx: PD
Mech: stimulate DA receptors (particularly D2) in striatum
AE: n/v, postural hypotension, dyskinesia, adverse behavioral effects, excessive daytime sleepiness, disorders of impulse control
Other: less likely to cause dyskinesia and motor fluctuations than levodopa

10

Trihexyphenidyl

mAChR antagonist
Indx: PD, drug-induced EPS
Mech: block mAChRs in striatum
AE: mAChR antag side effects (dry mouth, urinary retention, confusion, attacks of angle-closure glaucoma in suscept. pts)
Other: particularly useful treating tremor of PD, not indicated in elderly or demented patients

11

Selegiline

MAO-B inhibitors
Indx: PD; depression
Mech: inhibit MAO-B in brain, increases half-life of DA in brain; inhibit MAO, decreasing metabolism of NE and 5-HT
AE: nausea, headache; postural hypotension, sexual dysfunction, hypertensive crises, sleep disturbances, increased appetite (weight gain), hepatotoxicity

12

Amantadine

NMDAR antagonist
Indx: PD [and antiviral/prophylaxis for influenza]
Mech: uncertain; may decrease glutaminergic transmission in basal ganglia or simulate DA receptors/release
AE: CNS effects (dizziness, confusion), nausea, dermatological reactions

13

Tetrabenazine

VMAT2 antagonist
Indx: chorea, tics
Mech: inhibits uptake of DA into synaptic vesicles, depletes neuronal DA
AE: depression, drowsiness/fatigue, Parkinsonian syndrome

14

Haloperidol

Antipsychotics
Indx: chorea, tics
Mech: block D2 receptors
AE: EPS

15

Clonidine

a2 agonist
Indx: tics; neuropathic pain
Mech: May reduce activity of noradrenergic neurons in locus ceruleus; analgesic: stimulate a2 receptors in brain, spinal cord
AE: sedation, xerostomia, constipation; a2 agonist side fx (sedation, hypotension, dry mouth)

16

Botulinum toxin

Muscle relaxant
Indx: tics; neurogenic bladder due to spinal cord injury or MS
Mech: blocks exocytosis of ACh from cholinergic nerve terminals at NMJ, causes local muscle paralysis; same mech, causing dec. bladder tone and dec. incontinence
AE: injection site rxn, weakness of injected msc and adj msc; UTI, urinary retention, hematuria
Other: used for focal motor or vocal tics

17

Propranolol

Beta antagonist
Indx: essential tremor (drug of choice)
Mech: blocks beta receptors effects in brain and on SKM
AE: beta antag side effects (decreased HR, AV block, hypotension, exacerbation of asthma or COPD, impaired circ to hands/feet

18

Primidone

Antiepileptic drug
Indx: essential tremor
Mech: metabolized to phenobarbital, which binds to allosteric site on GABAa receptors in brain, spinal cord; increase GABA-mediated IPSP
AE: depression, drowsiness/fatigue, nausea

19

Topiramate

Antiepileptic (2nd gen)/anticonvulsant drug
Indx: essential tremor, neuropathic pain, seizures
Mech: prolongs inactivated state of Na channels, enhance GABAergic transmission
AE: cognition problems, weight loss, metabolic acidosis, nephrolithiasis, metallic taste, ocular problems, teratogenic effects (increased risk for cleft palate, etc)
Seizure indx: partial and generalized tonic-clonic

20

Gabapentin

Antiepileptic (2nd gen)/anticonvulsant drug
Indx: essential tremor, neuropathic pain, seizures
Mech: Binds to a2delta subunit of V-gated Ca channels in brain, spinal cord but mech for ET/analgesic is uncertain; may decrease glut release and/or enhance GABAergic trans
AE: ataxia, sedation, headache, weight gain, hyperactivity in children
Other: more efficient in treating neuropathic pain than seizures
Seizure indx: adjunct for partial and secondarily generalized tonic-clonic

21

Tropicamide

mAChR antagonist
Indx: facilitates ophthalmoscopy; facilitates refraction
Mech: block mAChRs on pupillary constrictor msc, causing mydriasis; block mAChRs on ciliary msc, causing cycloplegia
AE: photosensitivity, blurred vision, systemic mAChR antag side effects (xerostomia, confusion, etc.)

22

Phenylephrine

a1 agonist
Indx: facilitation of ophthalmoscopy
Mech: stimulates a1 receptors on pupillary dilator msc, causing mydriasis
AE: photosensitivity, systemic a1 agonist side effects (increased BP)
Other: preferred drug if patient needs to recover eye sight quickly

23

Dexamethasone

Glucocorticoid
Indx: vasogenic cerebral edema, CINV (with 5-HT antag and NK1 antag), PONV
Mech: inhibits PLA2 leading to improved function of damaged BBB
AE: iatrogenic Cushing's syndrome (insomnia, behavioral changes, peptic ulcers, truncal obesity, weight gain, muscle wasting, myopathy, hyperglycemia, diabetes, osteoporosis, etc.)

24

Mannitol

Osmotic diuretic
Indx: increased intracranial pressure
Mech: increases ECFosm, so shifts fluid from ICF to ECF
AE: overexpansion of ECF, electrolyte disturbances, rebound increased ICP due to drug entering BBB

25

Acetazolamide

Carbonic anhydrase inhibitor diuretic
Indx: idiopathic intracranial hypertension
Mech: inhibits carbonic anhydride, decreasing secretion of fluids driven by H+/HCO3- secretion, decreasing CSF production
AE: hypokalemia, metabolic acidosis

26

Ibuprofen

NSAID
Indx: mild to moderate pain, pyrexia, inflammation
Mech: inhibit COX, decrease synth of PGs
AE: GI side fx, decreased platelet aggregation leading to increased bleeding, decreased RBF and GFR in pts with decreased ECV
Other: can have hypersensitivity runs

27

Acetaminophen

NSAID
Indx: mild to moderate pain, pyrexia
Mech: inhibit COX, decrease synth of PGs
AE: GI side fx, decreased platelet aggregation leading to increased bleeding, decreased RBF and GFR in pts with decreased ECV
Other: can have hypersensitivity runs

28

Morphine

Full u agonist - opioid analgesic
Indx: moderate to severe pain
Mech: stimulate mu opioid receptors in amygdala, SN, periaqueductal gray area, rostroventral medulla, and spinal cord
AE: sedation, respiratory depression, constipation, n/v, urinary retention, histamine release (vasodilation, allergic sx), neuron doctrine effects (increased ADH secretion), risk of psych dependence and abuse

29

Fentanyl

Full u agonist - opioid analgesic
Indx: moderate to severe pain
Mech: stimulate mu opioid receptors in amygdala, SN, periaqueductal gray area, rostroventral medulla, and spinal cord
AE: sedation, respiratory depression, constipation, n/v, urinary retention, histamine release (vasodilation, allergic sx), neuron doctrine effects (increased ADH secretion), risk of psych dependence and abuse

30

Methadone

Full u agonist - opioid analgesic
Indx: moderate to severe pain; mgmt of opioid dependence
Mech: stimulate mu opioid receptors in amygdala, SN, periaqueductal gray area, rostroventral medulla, and spinal cord; agonist at mu opioid receptors
AE: sedation, respiratory depression, constipation, n/v, urinary retention, histamine release (vasodilation, allergic sx), neuron doctrine effects (increased ADH secretion), risk of psych dependence and abuse, drowsiness, inc. risk of cardiac arrhythmias

31

Codeine

Full u agonist - opioid analgesic
Indx: mild to moderate pain
Mech: stimulate mu opioid receptors in amygdala, SN, periaqueductal gray area, rostroventral medulla, and spinal cord
AE: sedation, respiratory depression, constipation, n/v, urinary retention, histamine release (vasodilation, allergic sx), neuron doctrine effects (increased ADH secretion), risk of psych dependence and abuse

32

Buprenorphine

Partial u agonist - opioid analgesic
Indx: moderate to severe pain; mgmt of opioid dependence (w/ naloxone)
Mech: stimulate mu opioid receptors in amygdala, SN, periaqueductal gray area, rostroventral medulla, and spinal cord; partial agonist at mu opioid receptor
AE: sedation, respiratory depression, constipation, n/v, urinary retention, histamine release (vasodilation, allergic sx), neuron doctrine effects (increased ADH secretion), risk of psych dependence and abuse, other opioid side fx

33

Naloxone

Opioid antagonist
Indx: opioid overdose; prevention of IV abuse of buprenorphine
Mech: blocks all opioid receptors
Other: works well in blocking effect of buprenorphine when used together

34

Naltrexone

Opioid antagonist
Indx: opioid overdose; mgmt of ethanol dependence
Mech: blocks all opioid receptors; inhibits rewarding effects of ethanol
AE: nausea, headache, dizziness
Other: useful for staying off opioids after withdrawal

35

Tramadol

Misc. analgesic
Indx: moderate pain
Mech: inhibit SERT and NET, weakly stimulate opioid receptors
AE: dizziness, n/v, constipation
Other: contraindicated in patients with seizures

36

Clonidine

a2 agonist
Indx: post-op pain management
Mech: stimulate a2 receptors in brain and spinal cord
AE: a2 agonist side fx (sedation, hypotension, dry mouth)

37

Carbamazepine

Anticonvulsant/antiepileptic (1st gen)
Indx: neuropathic pain, bipolar disorder, seizures
Mech: prolongs inactivated state of V-gated Na channels; mech for mood stability poorly understood
AE: diplopia, blurred vision, rash, leukopenia, hyponatremia, teratogenic effects; ataxia
Other: very useful in treating trigeminal neuralgia
Seizure indx: partial and secondarily generalized tonic-clonic

38

Phenytoin

Anticonvulsant/ antiepileptic (1st gen)
Indx: neuropathic pain, seizures
Mech: prolongs inactivated state of V-gated Na channels
AE: gingival hyperplasia, acne, hirsutism, facial coarsening, rash, teratogenic effects; nystagmus, dose-related cerebellar syndrome
Seizure indx: partial and generalized tonic-clonic

39

Amitriptyline

Antidepressant - TCA
Indx: neuropathic pain; anxiety (social anciety disorder, panic disorder), depression
Mech: inhibit NET and SERT, mech for analgesic effects uncertain
AE: mAChR antag side fx (dry mouth, urinary retention, confusion, etc.), a1 antag side fx (postural hypotension), H1 antag side fx (sedation, increased appetite leading to weight gain), cardiac arrythmias, conduction delays, etc)
Other: overdose leads to diagnostic triad of coma, seizures, ECG abnormalities (QT prolongation, etc); low therapeutic index

40

Duloxetine

Antidepressant - SNRI
Indx: neuropathic pain, anxiety (GAD), depression
Mech: inhibit SERT and NET, analgesic effect mech uncertain
AE: GI disturbances, sedation, sexual dysfunction
Other: can also be used for pain assoc with fibromyalgia and chronic MSK pain; may possible raise BP

41

What drugs can cause seizures in normal people?

Tramadol, bupropion, and (clozapine)

42

Bethanechol

mAChR agonist
Indx: Neurogenic bladder due to spinal bladder or autonomic neuropathy [overflow incontinence]
Mech: stimulates mAChRs in bladder, leads to increased bladder tone and increased emptying
AE: mAChR agonist side fx (GI side fx (craps, diarrhea, n/v), diaphoresis, hypersalivation, lacrimation, etc.)
Other: may cause bronchospasm/wheezing, caution in pts with asthma

43

Oxybutynin

mAChR antagonist
Indx: neurogenic bladder due to spinal cord injury or MS
Mech: Black mAChR in bladder, leads to decreased bladder tone and decreased incontinence
AE: mAChR antag side fx (xerostomia, confusion, attacks of angle-closure glaucoma, etc.)

44

Ondansetron

5-HT antagonist
Indx: chemo-induced NV, radiation therapy-induced NV, postop NV, gastroenteritis-induced NV
Mech: block 5-HT receptors on vagal afferents in GI tract, CTZ, EC/NTS, causes decreased NV
AE: headache, constipation, dizziness, increased QT interval

45

Metoclopramide

D2 antagonist
Indx: PONV, gastroenteritis-induced NV, migraine-induced NV, NV due to GI motility disorders, CINV
Mech: block D2 receptors in CTZ and EC/NTS, decreasing NV
AE: EPS

46

Scopolamine

mAChR antagonist
Indx: PONV, NV due to motion sickness/vestibular disorders
Mech: block mAChR on vestibular afferents and EC/NTS, decreasing NV
AE: mAChR antag side fx (xerostomia, constipation, urinary retention, visual disturbances, etc)
Other: contraindicated in pts with GI or urinary tract obstruction, BPH

47

Diphenhydramine

H1 antihistamine (1st gen)
Indx: PONV, NV due to motion sickness/vestibular disorders
Mech: Block H1 receptors on vestibular afferents and EC/NTS, decreasing NV
AE: mAChR antag side fx (xerostomia, confusion, urinary retention, constipation, visual disturbances)
Other: contraindicated in pts with GI or urinary tract obstruction, BPH

48

Acamprosate

GABA analog
Indx: Management of ethanol dependence
Mech: may decrease glutaminergic transmission and attenuate neuronal hyperexcitability
AE: diarrhea, nervousness, fatigue

49

Nicotine

nAChR agonist
Indx: mgmt of smoking cessation
Mech: suppress acute and prolonged withdrawal sx and cravings in nicotine-dependent pts
AE: headache, appetite stimulation

50

Varenicline

nAChR partial agonist
Indx: mgmt of smoking cessation
Mech: suppress acute and prolonged withdrawal sx and cravings in nicotine-dependent pts
AE: nausea, insomnia, headache, abnormal dreams, neuropsychiatric sx (agitation, depression, increased suicide risk)

51

Buproprion

NDRI
Indx: mgmt of smoking cessation; depression
Mech: inhibit NET and DAT (DA to attenuate cravings, NE to relieve withdrawal sx)
AE: insomnia, headache, agitation, xerostomia
Other: can cause seizures

52

Fluoxetine

SSRI
Indx: anxiety (GAD, PTSD, OCS, social anxiety disorder, panic disorder), depression
Mech: inhibit SERT
AE: Gi side fx (NV, GI cramps, diarrhea), sexual dysfunction, motor restlessness, insomnia

53

Buspirone

Anxiolytic (partial serotonin agonist)
Indx: anxiety (GAD)
Mech: partial agonist at 5-HT receptors
AE: dizziness, non-specific chest pain

54

Lithium

Indx: bipolar disorder
Mech: inhibits multiple enzymes involved in generation of secondary messengers (e.g. IP3, cAMP), but mech poorly understood
AE: tremor, weight gain, nephrogenic diabetes insipidus (polyuria), polydipsia, GI side fx, rash
Other: effective for mania

55

Divalproex

Antiepileptic (1st gen)
Indx: bipolar disorder, seizures
Mech: prolong inactive state of Na channels, block T-type Ca channels, mech for mood stabilization poorly understood
AE: weight gain, alopecia, tremor, teratogenic effects
Seizure indx: partial and generalized tonic-clonic, myoclonic, absence

56

Lamotrigine

Antiepileptic (2nd gen)
Indx: bipolar disorder, seizures
Mech: prolong inactive state of Na channels, inhibit glutaminergic transmission, block T-type Ca channels, mech for mood stabilization poorly understood
AE: rash, ataxia, headaches, diplopia
Seizure indx: partial and generalized tonic-clonic, myoclonic, 2nd line for absence

57

Quetiapine

2nd gen antipsychotic
Indx: bipolar disorder
Mech: block D2 and 5-HT receptors, mech for mood stabilization poorly understood
AE: weight gain, metabolic changes, EPS, sedation

58

Ethosuximide

Antiepileptic (1st gen)
Indx: seizures
Mech: block T-type Ca channels
AE: sleep disturbances, rash
Seizure indx: absence

59

Phenobarbital

Antiepileptic (1st gen)
Indx: seizures
Mech: binds to allosteric site on GABAa receptors in brain, spinal cord, increases GABA-mediated IPSPs
AE: psychomotor impairment, tolerance, physical dependence, abuse potential, daytime sedation, adverse effects on sleep cycle
Seizure indx: partial and secondonary generalized tonic-clonic; used now for children and status epilepticus

60

Primidone

Antiepileptic (1st gen)
Indx: seizures
Mech: metabolized to phenobarbital
AE: psychomotor impairment, tolerance, physical dependence, daytime sedation, adverse effects on sleep cycle
Seizure indx: partial and secondarily generalized tonic-clonic

61

Levetiracetam

2nd gen antiepileptic
Indx: seizures
Mech: may modify exocytosis of glutamate and GABA via an effect on vesicular function
AE: psychosis, hallucinations, irritability
Seizure indx: partial and gernealized tonic-clonic, myoclonic, 2nd line for absence

62

Drugs for neuropathic pain

Dying Axons Can Get Cured To Lower Pain
Duloxetine
Amtriptyline
Clonidine
Gabapentin
Carbamazepine
Topiramate
Lidocaine
Phenytoin

63

Drugs for tremor

Tremors Get Bad, Poor Prognosis
Topiramate
Gabapentin
Benzodiazepine
Primidone
Propanolol

64

Drugs for tics

Tics Can Be Highly Repetitive
Tetrabenazine
Clonidine
Botox
Haloperidol
Risperidone

65

Drugs for chorea

chorea is HOT
Haloperidol
Olanzapine
Tetrabenazine

66

Drugs for nausea/vomiting

Only Male Donkeys Do Big Shit
Ondansetron
Metoclopramide
Dexamethasone
Diphenhydramine
Benzodiaepines
Scopolamine

67

Drugs for neurogenic bladder

BOB
Bethanechol
Oxybutynin
Botox

68

Drugs for bipolar disorder

Lame Ladies Quit Dealing with Crazies
Lithium
Lamotrigine
Quetiapine
Divalproex
Carbamazepine

69

Drugs for anxiety

Fuck Benz, Drive a Bus
Fluoxetine
Benzodiazepine
Duloxetine
Amitriptyline
Buspirone

70

Drugs for Alzheimer's disease

MD for AD
Memantine
Donepezil