Semester Cumulative Gen Pharm Review

tamoxifen

• type: selective estrogen receptor modulator

• indication: prevention & tx of breast cancer

• MoA: competitive partial agonist inhibitor of estradiol → inhibition of estrogen

• SE:

  • crystalline maculopathy

  • macular edema

  • whorl keratopathy

  • increased risk of blood clots

topiramate

• type: anticonvulsant

• indication:

  • migraine tx

  • weight loss tx

  • epilepsy

• MoA: blockage of voltage gated Na channels, GABA agonist, glutamate kainite & AMPA receptor blocker → decreased neuron firing

• SE:

  • idiosyncratic drug rxn

  • nystagmus

  • diplopia

  • blurry vision

  • appetite suppression/weight loss

tamsulosin (terazosin, prazosin, doxazosin)

• type: alpha 1 blocker

• indication: tx for benign prostatic hypertrophy

• MoA: alpha 1 receptor block → smooth muscle relaxation → vasodilation

• SE:

  • intraoperative floppy iris syndrome

  • nausea

  • dizziness

  • reflex tachycardia

  • orthostatic hypotension

  • HA

  • flushing

edrophonium, pyridostigmine, neostigmine, physostigmine

• type: reversible, indirect cholinergic agonist

• indication: diagnosis & tx of myasthenia gravis

• MoA:

  • binds & inhibits acetylcholinesterase → increases ACh in synapse & NMJ

• SE:

  • sweating

  • increased saliva

  • increased urination

  • increased GI motility

  • miosis

  • increased accommodation

  • increased lacrimation

  • retinal detachment

  • decreased IOP

  • muscle cramps & weakness

  • bradycardia

  • asthma/COPD

edrophonium

what drug is used to diagnose myasthenia gravis & does not cross BBB?

pyridostigmine/neostigmine

what drug is used to treat myasthenia gravis & does not cross BBB?

physostigmine

what drug is used in an atropine overdose & can cross the BBB?

echothiophate

• type: irreversible indirect cholinergic agonist

• indication: decreases IOP in glaucoma (rare usage)

• MoA: covalently binds & inhibits acetylcholinesterase → increased ACh

• SE:

  • sweating

  • increased saliva

  • increased urination

  • miosis

  • increased accommodation

  • increased lacrimation

  • retinal detachment

  • decreased IOP

  • skeletal muscle cramps/weakness

  • bradycardia

  • asthma/COPD

diarrhea, urination, miosis, bradycardia, emesis, lacrimation, lethargy, salivation

what are the signs of indirect cholinergic agonist overdose?

atropine

what drug is given for an indirect, reversible cholinergic agonist overdose?

pralidoxime

what drug is given for an indirect, irreversible cholinergic agonist overdose?

phenothiazines: chlorpromazine, thioridazine

• typical, 1st gen anti-psychotic

• indications:

  • schizophrenia

  • depression, BP

  • anti-emetic

• MoA: dopamine receptor antagonist

• SE:

  • corneal endothelium pigmentation

  • anterior stellate cataracts

  • RPE pigmentation disruptions

  • oculogyric crisis

haloperidol

• typical, 1st gen anti-psychotic

• indications:

  • schizophrenia

  • depression, BP

  • anti-emetic

• MoA: dopamine receptor antagonist

• SE:

  • oculogyric crisis

  • no pigment effects

aripiprazole

• atypical, 2nd gen anti-psychotic

• MoA: dopamine receptor antagonist

• SE:

  • no ocular pigment changes

  • less Parkinson’s like movement issues

  • akathisia

  • diabetes

  • weight gain

hydroxychloroquine

• indication:

  • anti-malarial classification

  • used to tx autoimmune disorders like RA & lupus

• MoA: phospholipase A2 inhibitor

• SE:

  • whorl keratopathy

  • bullseye maculopathy

  • risk of renal toxicity

  • VF loss

  • decreased vision/contrast sensitivity

  • color vision changes

>5.0mg/kg/day

what is the daily dose of hydroxychloroquine that increases risk for renal toxicity?

tamoxifen

concurrent use of hydroxychloroquine & ______ increases the risk of renal toxicity 5x

rifampin

• indication: active & latent TB

• MoA: binds to beta subunit of DNA dependent RNA polymerase

• SE:

  • hepatotoxicity

  • orange-pink discoloration of urine & tears

  • exudative conjunctivitis

amitriptyline, imipramine

• TCA

• MoA: blocks reuptake of serotonin & NE in presynaptic terminals

• SE:

  • anti-cholinergic

  • dry eye

  • increased IOP

  • mydriasis

  • can precipitate angle closure

pseudoephedrine

• OTC decongestant

• MoA:

  • mixed acting adrenergic agonist

  • increases sympathetic effects

  • binds directly to alpha & beta receptors

  • taken into presynaptic neuron via NE transporter → packaged into vesicles & released into synapse

• SE:

  • mydriasis

  • dry eye

  • decreased accommodation

  • slight eyelid raise

  • decreased eye redness

  • increased IOP

  • tachycardia

  • bronchodilation

cocaine

• DEA controlled substance schedule 2

• stimulant

• MoA:

  • blocks reuptake of NE & DA → increases sympathetic effects

  • blocks Na channels in neurons → anesthetic effects

• SE:

  • mydriasis

  • keratitis

  • reduced blink

  • corneal ulcers

  • crack cornea

  • tachycardia

  • bronchodilation

carbidopa-levodopa

• indication: Parkinson’s tx

• MoA: increases synthesis of DA

• SE:

  • mydriasis

  • hallucinations or psychotic behaviors

  • nausea

bromocriptine

• indication: prolactin secreting pituitary adenoma tx

• MoA: DA agonist

• SE:

  • mydriasis

  • hallucinations or psychotic behaviors

  • nausea

amantadine

• indication: Parkinson’s tx

• MoA: increases release of DA

• SE:

  • mydriasis

  • hallucinations or psychotic behaviors

  • nausea

cyclosporine

• chemotherapeutic agent

• MoA: inhibits release & production of IL-2 → helps prevent organ transplant rejections

• SE:

  • opportunistic injections

  • reversible posterior leukoencephalopathy syndrome

  • HA

  • altered consciousness

  • seizures

  • visual disturbances: aura, visual hallucinations, hemianopsia, cortical blindness

ergotamine, sumatriptan, zolmitriptan

• MoA: serotonin 5-HT1 receptor agonist → vasoconstriction of pial/dural vessels, inhibit release of pain mediators, inhibition of trigeminal nerves

• SE:

  • blood clots → NAION, CRAO/CRVO, heart attack/stroke

amiodarone

• indication: arrhythmias

• MoA: K channel blocker (also Na & Ca)

• SE:

  • lots of drug interactions

  • whorl keratopathy

  • anterior subcapsular lens deposits/cataracts

  • NAION

  • thyroid dysfunction

  • torsades des points

tramadol

• analgesic

• DEA controlled substance schedule 4

• MoA: Mu opioid receptor agonist, inhibits reuptake of serotonin & NE

• SE:

  • dry mouth

  • sedation, dizziness

  • nausea, constipation

  • respiratory depression

  • seizures

  • serotonin syndrome

  • miosis w/ OD

  • potential for tolerance, physical dependence, withdrawal, addiction

  • immune suppression

  • itching

• contraindications:

  • other CNS depressants

  • asthma, COPD, sleep apnea

  • kidney/liver disease

  • closed head injury

  • history of addiction

naloxone

• short & fast acting opioid receptor antagonist

• used to tx opioid OD

• binds to opioid receptor but blocks it

• rapidly reverses opioid effects

• antagonist precipitated withdrawal