Bolded Drugs Flashcards
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
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
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
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]
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]
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
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
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
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
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
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
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
Tetrabenazine
VMAT2 antagonist
Indx: chorea, tics
Mech: inhibits uptake of DA into synaptic vesicles, depletes neuronal DA
AE: depression, drowsiness/fatigue, Parkinsonian syndrome
Haloperidol
Antipsychotics
Indx: chorea, tics
Mech: block D2 receptors
AE: EPS
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)
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
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
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
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
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
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.)
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
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.)
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
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
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
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
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