Pharm Exam 1 Flashcards
What is the function of Cholinergic agents in dealing with Glaucoma?
- Open-angle glaucoma: contraction of ciliary muscles leading to increase flow through the intertribecular spaces
- Closed Angle Glaucoma: contraction of the sphincter muscles increases the angle between the sclera and the iris
What are some example of cholinergic agents?
-Carbachol,, pilocarpine, echothiophate
What are some adverse reactions of carbachol, pilocarpine, physostigmine, and ecothiophate?
- Carbachol- over stimulation of nicotinic receptors
- Pilocarpine - HTN and tachycardia
- Physostigmine- (can cross the BBB) seizures and abnormal defecation
- Ecothiophate- night blindness and frontal headache
What are the action of Beta adrenergic blockers in glaucoma?
- They interact with ciliary epithelium to decrease production of aqueous humor. No effect on outflow.
What are some examples of beta blockers used in chronic open-angle gluacoma?
Timolol, carteolol, betaxolol
What are the adverse effects of Timolol, Carteolol, Betaxolol?
- Timolol: blurred vision, dry eyes, hallucination
- Carteolol: insomnia, bronchospasm
- Betaxolol: MI, AV block
What is the mechanism of action of Prostaglandin analogs in open-angle glaucoma and intraocular hypertension?
- increase the outflow of the uveoscleral aqueous humor (latanoprost) as well as the outflow through the trabecular meshwork (bimatoprost)
Name the Prostaglandin analogs used in intraocular hypertension and open-angle glaucoma?
- Latanoprost, bimatoprost, travoprost
“-prost”
What are some adverse effects of prostaglandin analogs?
- darkens color of the iris
- macular retinal edema
- conjunctival hyperemia (bimatoprost, travoprost)
What is the mechanism of action of carbonic anhydrase inhibitors in the treatment of intraocular hypertension and open-angle glaucoma?
- Decrease aqueous humor production
- No effect on pupils or vision
What are carbonic anhydrase inhibitors?
- Acetazolamide, brinzolamide, dorzolamide
“-amide”
What are the adverse effects of carbonic anhydrase inhibitors?
- Metabolic acidosis **
- Urolithiasis - high pH in urine
- electrolyte imbalance (acetazolamide)
- Agranulocytosis and thrombocytopenia (acetazolamide)
- Immune hypersensitivity reactions (dorzolamide)
- Burning sensation in the eye (dorzolamide)
What is the mechanism of action of Alpha-2 selective agonists in treating open-angle glaucoma?
- decrease production and increase outflow of aqueous humor
- Brimonidine - decreases aqueous humor production increase uveoscleral outflow
What drugs are alpha-2 selective agonists?
- Apraclonidine and brimonidine
What are the adverse effects that might result from use of alpha-2 selective agonists?
- irregular heart rate, fatigue, dry mouth, red, itchy, or swollen eyes
- Depression, dizziness, and chest pain with apreaclonidine
What is the mechanism of action of epinephrine?
- decreases aqueous humor production due to vasoconstriction and decrease blood flow to ciliary bodies.
What is the mechanism of action of dipivefrin?
a prodrug that is hydrolyzed to epinephrine within the eye.
What are adverse effects of dipivefrin and epinephrine?
- dipivefrin - burning sensation in the eye, follicular conjunctiva
- epinephrine- mydriasis, stinging, not to be used in closed-angle glaucoma
What is the serotonin theory?
Increases in urine 5-IAA levels and decrease in plasma serotonin levels–> most anti-migraine drugs are either serotonin agonist or antagonist.
- reserpine or fenfluramine causes an increase risk of attack
What is the mechanism of action of NSAIDS?
- Decrease the pain threshold secondary to decreasing prostaglandin synthesis.
What types of NSAIDS are used for migraine treatment?
- indomethacin,ibuprogen, aspirin, naproxen
What are some side effects of NSAIDS?
- ulcers, GI bleeding, and rebound headaches
What type of migraine and what is the mechanism of action of triptans?
- acute migraine treatment
- Block the release of pro-inflammatory neurotransmitters within the perivascular space in the vicinity of the trigeminal nerve.
What are the triptans that we need to know.
- anything with “-triptan”
- Sumatriptan, rizatriptan, naratriptan, almotriptan, frovatriptan, electriptan, and zolmitriptan.
What is contraindicated with Triptan use?
- concurrent ergot alkaloids use,
- coronary artery disease, ischemic disease
- MAO inhibitors use
What are the side effects of Triptan use?
- asthenia, fatigue, pain in neck, chest of jaw
What is different about second generation triptans and what are they?
- low adverse effect profile and faster onset of actions
- natratriptan, zolmitriptan, electriptan, almotriptan, rizatriptan, and frovatriptan
What is the mechanism of action of Opoids?
- decrease pain sensation secondary to agonist effects at U, K, and delta receptors
What is a type of opoid used for migrane?
- codeine
What type of migrane is acetaminophen used on and what can be done to make it stronger?
- headache - especially when aspirin is contraindicated. Only viable action during pregnancy.
- for moderate headache combine with isometheptene and dichlorophenazone
- for severe headaches combine with butalbital
When is butorphanol used and what is it’s MOA and adverse effect?
- intranasal spray for migraines
- MOA: partial agonist u and k
- AE: sedation confusion, and dizziness
When and how is meperidine used?
- Meperidine is used for SEVERE migraine pain and it is administered via IV
What is oxycodone and hydrocondone used and what is the main concern?
- used for severe pain, but addiction liability is worrisome
What is Metoclopramide used, what is its AE?
- Used in combination for migraines
- AE: galactorrhea, constipation, extrapyramidal effects, tardive dykinesia.
What are the uses and what are the adverse effects of Chlopromazine and prochlorperazine?
- Clinical uses: anti-emetic, schizophrenia, tourettes’s syndrome, huntington’s chorea and dementia
- AE: poikilthermic, blurred vision, constipation, agranulocytosis, phototoxicity
What is Amidrine?
A combo of acetaminophen, dichloralphenazone (analgesic and anti-pyretic), and isometheptene (vasoconstrictor)
What drugs are considered for migraine prophylaxis?
- Propranolol, pizotifen, tricyclic anti-depressants ( amitriptyline, dothiepin, and nortriptyline), Topiramate, Valproic acid, Gabapentin, Methysergide.
What is propranolol used for, what is its MOA, what are the Adverse effects, and what are the contraindication?
- Migraine prophylaxis, hypertension,
- MOA: B-blocker
- AE: bronchospasm, AT block, postural sym, sedation
- Contraindicated: asthmatic patients
What is the clinical uses of Pizotifen, AE, Contraindication?
- Clinical uses: RECURRENT migraine headaches, or when beta blockers are contraindicated
- Adverse effects: weight gain, antidepressants, anti-muscarinic effects
- Contra: MAO inhibitors use
What are the clinical uses of tricyclic anti-depressants (amitriptyline, dothiepin, and nortriptyline), what are the adverse effects, contraindication?
- uses: migrain prophylaxis
- AE: AV bundle branch block
- may precipitate mania in patients with bipolar
What is the clinical uses of Topiramate, what are its adverse effects?
- migraine prophylaxis, generalized tonic clonic, and partial seizures
- AE: p450 inducer therefore metabolism is induced by carbamazepine and phenytoin
- MOA: blocks Na+ channels and enhances GABA transmission
What is clinical uses of Valproic acid, MOA, AE?
- uses migraine prophylaxis, and generalized and absence seizures
- MOA: stabilizes Na+ channels in the inactive state and inhibits low-threshold T-type Ca2+ thereby increasing GABA transmission.
- AE: Drowsiness, weight gain, bone marrow depression
What is the clinical uses of Gabapentin, MOA, and AE?
- Uses: migraine prophylaxis, partial seizures
- MOA: analoge of GABA
- AE: dizziness, sedations, and peripheral edema
What is the clinical uses of Methysergide, MOA, AE?
- Uses: highly effective migraine prophylaxis, used for severe refractory migraines or cluster headaches
- MOA: Serotonin antagonists
- AE: retroperitoneal fibrosis, fibrosis of heart valves, and pleura
What are the functions of the mu receptor?
- Supraspinal and spinal analgesia
- Sedation and inhibition
What are the function of the delta receptor?
- Supraspinal and spinal analgesia, modulation of hormones and neurotransmitter release
What are the functions of the kappa receptor?
- Psychomimetic effects, supraspinal and spinal analgesia
Where and what does Codeine get metabolized into?
What is a more potent widely used derivative of morphine?
- Codein hepatic de-amination to morphine
- Hydromorphone
When is morphine used and what is a possible AE of methadone?
- Long plasma half-life used mostly for chronic pain in terminally ill cancer patients.
- AE: respiratory depression
What are the uses and possible AE of Meperidine?
- uses: analgesic efficacy - less potent though.
- AE: seizures,
- causes mydriasis (dilation) rather then miosis (constriction) as seen in opiods
What is the uses of butorphanol?
- agonist at K and partial agonist at u
- analgesia with milder euphoria
- treat opioid addiction, maintenance of anesthesia, labor pain
What is the uses of Buprenorphine?
- Pain, chronic
What is the use of Nalbuphine? What is the AE?
- effective analgesic, pre-op, post-op, obstetrical analgesia,
AE- Depression
What is an antidote for opioid intoxication due to its antagonist effects at mu receptors and K receptors?
-Naloxone
What is naltrexone used for?
A pure competitive antagonist that is used for opioid dependence and specifically alcohol withdrawal.
What type of signaling is partially mediated when achieving tolerance with opioids?
-NMDA signaling
What effects can occur with the increased opioid usage?
- REspiratory depression (decreased sensitivity of chemo-sensitive neurons to pCO2)
- GI disturbances: inc tone of pyloric sphincter and decreased peristaltic movement
- Miosis
- Nausea and vomiting
- Hypotension and bradycardia- impairment of sympathetic compensatory responses
What are 3 drugs that you can give for treatment of chronic pain not responsive to opioids?
- Amitriptyline, nortriptyline, and imipramine
What are 2 NMDA receptor antagonists that you can give for pain?
-Ketamine (acute severe pain) and dexamethorphan (chronic pain and post-op)
What are adrenergic agonists?
- Clonidine, Gabapentin, pregabalin, lamotrigine, carbamazepine
What types of pain does clonidine treat?
- Acute and chronic pain
What type of pain does Gabapentin treat?
Chronic and post-op pain.
What are the uses of pregabalin and what is the MOA?
- neuropathic pain, fibromyalgia, and spinal cord injury
- GABA analog, more potent, faster, and predictable than gabapentin
What is Lamotrigine used for?
- Trigeminal neuralgia and neuropathic pain.
- AE: skin reaction
What is carbamazepine used for and what is its MOA?
- trigeminal neuralgia
- Na+ channel blocker
What are the different types of dementia?
- Alzheimer’s dementia
- Vascular dementia
- Lewy body dementia
- Frontal temporal dementia
- HIV- associated dementia
What drugs class would you use for depression associated with Alzheimer’s Disease?
- SSRI’s (sertraline, fluoxetine)
- Tricyclic antidepressants (caution)
What medications would you use to treat hallucinations associated with Alzheimer’s Disease?
- Quetiapine, olanzepine, risperidone
What drug is the most popular to treat delusions associated with alzheimer’s disease?
- Haloperidol
What 3 Cholinesterase inhibitors would you use to treat Alzheimer’s Dementia?
- Donepezil, Rivastigmine, Galatamine
What are some characteristics of Donepezil?
What AE might appear?
- long plasma half-life, lower affinity for peripheral cholinesterase (less secondary side effect)
AE: cholinergic side effects (diarrhea, nausea, and vomiting)
What must you administer Rivastigmine with?
What are possible AE?
- Must be administered with food
- significant nausea vomiting, headaches, anorexia.
