Neuro Drugs Flashcards
What is the acute treatment for tension headaches?
1) NSAIDs
2) Caffeine
3) Butalbital (barbiturate)
MOA of Butalbital
1) Facilitaes GABA neurotransmission
MOA of Caffeine
1) Acts as a competitive antagonists for adenosine receptor
What is the prophylactic treatment for tension headaches? How long do these drugs take to work?
1) Older anti-depressants
2) 2-6 weeks to be efficacious
What are the three older antidepressants used for prophylactic treatment of tension headaches?
1) Amitriptyline
2) Doxepin
3) Imipramine
What is the MOA of Sumatriptan?
1) 5-HT1 b/d agonist; also known as triptan class
Which 5-HT1 b/d agonist has the slowest time to onset?
1) Naratriptan
What is the physiological effect of 5-HT1 b/d (triptans)?
1) Cause the inhibition of the release of vasodilators substance P and CGRP
What are the adverse effects of 5-HT1 b/d triptans?
1) Altered sensation
2) Pain at injection
3) Chest discomfort
What are the three contraindications of triptans?
1) Coronary artery disease
2) Uncontroled HTN
3) Prinzmetal angina
What is given to pt who has Sjogren’s syndrome?
1) Pilocarpine- direct cholinomimetic
Why should triptans and ergots, both drugs used to treat migraines, should never be used together?
1) Both have a vasoconstrictive effect
What is the treatment for migraine headaches?
1) NSAIDs
2) Triptans or Ergots
3) Dopamine Antagonists (D2)
What is the adverse effect of D2 Antagonsits?
1) Result in blockage of dopamine receptors in the basal ganglia
2) Causes parkinsonisms, dystonias, and neuroleptic malignant syndrome
Inability to sit; restlessness
Akathisia
What is the drug used initially for Parkinson’s?
1) MAO-B inhibitors (-gilines)
2) Selegiline and Rasagiline
Non-selective MAO inhibitors?
1) Red wine
2) Aged cheese
Why should non-selective MAOs not be used for the treatment of parkinson’s?
1) They will cause hypertensive crisis when combined with L-DOPA
What are the Dopamine agonists used to treat Parkinson disease?
1) Pramipexole (D3 agonist)
2) Ropinirole (D2 agonist)
Biperiden
Trihexyphenidyl
Benztropine
Centrally acting Anti-muscarinics
What are the side effects of anti-muscarinics?
1) Dry mouth
2) Urinary retention
3) Constipation
Pramipexole
Ropinirole
Dopamine agonists
What are contraindications for amantidine?
1) Seizures
2) Congestive heart failure
What is the window of effectiveness for L-DOPA? Why is L-DOPA used last in the treatment for Parkinson?
1) 5 years
2) Once L-DOPA is ineffective, treatment becomes extremely difficult
What is always given with L-DOPA? Why?
1) Carbidopa
2) Carbidopa inhibits the formation of peripheral dopamine resulting in L-DOPA use at lower doses
Why can’t Phenothiazine be used for treatment of L-DOPA induced nausea?
1) Phenothizine is a dopamine receptor antagonist resulting in increased Parkinson
Entacapone
COMT inhibitor
What are the adverse effects of L-DOPA?
1) Nausea and vomiting
2) Arrhythmias
3) Dyskinesia
4) Behavior change
What are the treatments for Myasthenia gravis?
1) Immunosuppressants
2) Plasmapheresis
3) Anticholine esterase
What are the immunosuppressants used in Myasthenia gravis?
1) Azathioprine
2) Cyclosporine
3) IV immunoglobulin
MOA of Azathioprine
1) Converted to mercaptopurine which inhibits cell proliferation by interfering with purine metabolism
Neostigmine
Pyridostigmine
Quaternary Anti-choline esterase
What must Quaternary anticholine esterases be given with?
An anti-muscarinic due to the increase in cholinergic neurons at other sites
GABA analogue for GABA-B receptor; useful for MS, Spinal injury, and ALS
Baclofen
MOA of Diazepam
Increases GABAnergic neurotranmission
MOA of Tizanidine
1) Analouge of clonidine
2) Reinforces inhibitory effects in spinal cord (alpha 2 agonist)
MOA of Riluzole
1) Inhibits glutamate release
2) Used for ALS and to delay tracheostomy
MOA of Gabapentin
1) Increases release of GABA
2) Also used for peripheral neuropathy pain reduction
MOA of Dantrolene
Skeletal muscle relaxant by interfering with release of calcium ions
MOA of Baclofen
1) GABA-B agonist
Adverse effects of Baclofen
Drowsiness
What in general is the adverse effects of GABAergic drugs?
1) Drowsiness
Describe the Tensilon test
1) Used to determine treatment effectiveness
2) Use Edrophonium
3) Improvement = under dosed
4) Worsening = over dose (cholinergic crisis)
What are the indications and contraindications for Na channel blockers?
1) Indications: generalized tonic-clonic and focal seizures
2) Contraindications: Absence seizures (makes them worse)
What are Calcium ion channel blockers indicated for? Contraindicated?
1) Indications: simple absence seizures
2) Contraindications: Generalized tonic-clonic seizures
What are the adverse effects of valproate?
1) GI epigastric distress
2) Hepatic damage
3) Teratogenic (cause neural tube defects)
What are the adverse effects of Lamotrigine?
1) May induce Stevens-Johnson syndrome
2) Insomnia
3) Nightmares and vivid dreams
What two drugs are effective against all types of seizures?
1) Valproate
2) Lamotrigine
What type of seizure should a Na channel drug never be given to?
1) Absence seizures
2) Makes seizure worse
What are the three first line drugs used for generalized seizures?
1) Valproate
2) Lamotrigine
3) Topiramate
What anti-epileptic drug causes bone marrow depression?
Carbamazepine
What are the first line drugs for focal seizures?
1) Lamotrigine
2) Carbamazepine and Oxcarbazepine
3) Phenytoin
4) Levetiracetam
Epileptic drug that has first order elimination in low to mid therapeutic range and zero order elimination in high therapeutic range?
1) Phenytoin
What are the clinical findings of Phenytoin drug toxicity?
1) Cerebral and vestibular symptoms
2) Gingival hyperplasia
3) Osteomalacia
4) Teratogenic
What are the teratogenic effects of phenytoin?
1) Cardiac damage
2) Cleft palate
What anti-epileptic drug if administered wrong could results in Stevens-Johnson syndrome?
1) Lamotrigine
What anti-epileptic drug is also used to treat obesity?
Topiramate
What is the first line treatment for Typical Absence seizures?
1) Valproate
2) Ethosuximide
Zonisamide
Tiagabine
Gabapentin
Lacosamide
Adjunct drugs for Focal seizures
What is the drug of choice for status epilepticus?
Lorazepam
Why must Lorazepam be given quickly when given IV?
1) Because it causes respiratory and cardiovascular depression
MOA of Lorazepam
Enhances the neurotransmission of GABA-A synapse
MOA of Ethosuximide
Blocks T-type Ca channels of thalamic neurons
What are the indications for the use of tPA with stroke?
1) Acute Stroke that occurred less than 3 hours
2) CT scan shows no hemorrhage or edema
3) >18 years old
What are contraindications for the use of tPA?
1) Stroke symptoms lasting longer than 3 hours
2) Thrombocytopenia
3) Use of heparin
4) Prior stroke within 3 months
5) Major surgery
6) No witness to onset
What is the MOA of corticosteroids?
1) Reduce the formation of leukotrienes and prostaglandins by inhibiting phospholipase 2 (PLA2)
2) Causes suppression and redistribution of leukocytes
What drug inhibits phospholipase 2 (PLA2)
Corticosteroids
What is the treatment of choice for an acute MS attack?
3-5 day treatment of corticosteroids
What are the drugs used to treat MS attacks?
1) Corticosteroids
2) Plamsapheresis
3) IV immunoglobulins
4) Dimethyl fumarate
What drugs acts both to reduce MS attacks and disease progression?
Dimethyl fumarate
What are adverse effects of IFN beta-1a and 1b?
1) Injection site inflammation
2) Depression
3) Flu syndrome
4) Eventually doesn’t work
5) Formation of neutralizing antibodies
What type of IFN drug has an increased occurence for production of antibodies against it?
IFN beta 1b
What are the adverse effects of Glatiramer?
1) Injection site irritation
2) Transient reactions after several months (urticaria, flushing face, chest pain, dyspnea)
What drugs are disease modifying for MS?
1) INF 1a and 1b
2) Glatiramer
3) Fingolimod
4) Mitoxantrone
5) Natalizumab
6) Teriflunomide
Chemotherapy agent used for the treatment of MS; intercalates with DNA, RNA, and inhibits topoisomerase II
Mitoxantrone
What are the adverse effects of Mitoxantrone?
1) Cardiotoxicity
2) Acute Myelogenous Leukemia
Monoclonal antibody that reduces movement of immune cells into CNS; decreases the frequency of relapses
Natalizumab
Adverse effects of Natalizumab
1) Increased incidence of Progressive multifocal leukoencephalopathy
Adverse effects of Fingolimod
1) Influenza syndrome
2) Headache
3) Diarrhea
4) Shortness of breath
5) Bradycardia
6) Optic neurtis
Active metabolite of lufunomide; oral immunomodulator
Teriflunomide
MOA of Teriflunomide
Reversibly inhibits dihydroorotate dehydrogenase
MOA of glatiramer
Unknown but believed to be involved with the conversion of TH1 to TH2
What is the function of dimethyl fumarate?
1) Immunomodulatory without being immunosuppressed
2) Activation of antioxidant genes
What are the adverse effects of dimethyl fumarate?
1) Decreases lymphocyte count
2) May cause eczema if given topically at low doses
What happens if an anti-TNF is given to a pt. with MS?
1) Anti-TNF causes greater severity and frequency of MS attacks
What drug is approved for all severe forms of dementia?
Donepazil
Drugs approved for mild and moderate dementias
1) Donepazil
2) Galantamine
3) Rivastigmine
Drug that inhibits both acetylcholine esterase and butyrylcholine esterase
Rivastigmine
What should rivastigmine never be given with?
Muscle relaxant (succinylcholine)
What are the adverse effects of anti-choline esterase inhibitors?
Think DUMBBELLS
1) Diarrhea
2) Urination
3) Miosis
4) Bronchorrhea
5) Bradycardia
6) Emesis
7) Lacrimation
8) Salivation/sweating
NMDA uncompetitive antagonist
Memantine
MOA of Memantine
1) uncompetitively competes with Mg to reduce the influx of Ca
Adverse effects of memantine
1) Constipation
Adverse effects of Rivastigmine, Galantamine, or Donepazil
Diarrhea
When does an anticholine esterase drug have more effect in alzheimers?
Further in progression of disease
What are the least tolerated drugs in dementia pt. and make them worse?
1) Anti-cholinergics
2) Old anti-histamines
3) Anti-psychotics
4) Benzodiazepines
Where do dopamine antagonists work?
1) Mesolimbic system
2) Extra-pryamidal
3) Tubero-infundibular
4) Brainstem
Where does excess dopamine manifest most?
Mesolimbic system
1) Causes psychosis
Adverse effects of first generation antihistaminics (H1)
1) muscarinic blockade (blurry vision, dry mouth, urinary retention)
2) serotonergic blockage (Appetite stimulation)
3) alpha adrenergic (postural dizziness)
4) Cross blood brain barrier and cause sedation and cognitive dysfunction
Hydroxyzine
Promethazine
Chlorpheniramine
Diphenhydramine
First generation antihistamines
First line treatment for essential tremors?
Propranolol
Treatment for trigeminal neuralgia?
Carbemazepine
Treatment for unknown meningitis in 2 month old?
1) Ceftriaxone (3rd gen) - Treatment for N. meninigitidis and Group B Strep
2) Ampicilin - treatment for Listeria
Pt. presents with confusion, disoritentation in a tool shed. Excessive lacrimation, wheezing, flushed skin and sweating profusely
Acetylcholine poisoning due to Organophosphate (peseticide poisoning) inhibiting cholineesterase
Irreversible cholineesterase inhibitor
Organophosphates (pesticide)
Treatment for organophosphate poisoining
1) atropine (muscarinic antagonist)
MOA of Morphine
1) Mu agonist
2) Causes activation of potassium channels
What is the goal of treating glaucoma?
1) Decrease intraocular pressure via decreasing the amount of aqueous humor (Increase drainage or decrease synthesis)
Drug that decreases aqueous humor synthesis via inhibiting the carbonic anhydrase
1) Acetazolamide
Drugs that inhibit aqueous humor synthesis
1) alpha agonists (Epinephrine and brimonidine)
2) beta blockers (Timolol, betaxolol)
3) Acetazolamide
What are the adverse effects of using epinephrine and Brimonidine?
1) Mydriasis (DO NOT USE in Closed angle glaucoma)
2) Blurry vision
What should you never give to a pt. with closed angle glaucoma?
Any drug that causes Mydraisis (eye dilation)
What drugs increase the outflow of aqueous humor
1) Pilocarpine and carbachol (contract ciliary muscles and open trabecular meshwork)
2) Physostigmine and Echothiophate (indirect)
3) Latanoprost (prostaglandin)
MOA of Opioids
1) Inhibits the release of ACh, NE, 5-HT, glutamage
2) Opens K channels and closes Ca channels –> synaptic transmission
Most lipophilic opioid that is given as a dermal patch
Fentanyl
Opioid used for migrane
Butorphanol
What do all of these do?
Tiagabine
vigabatrin
Gabapentin
Increase effects of GABA
MOA of Barbiturates
Think: BarbiDURATes = duration
Facilitate GABA action by increasing duration of Cl channel opening, thus decreasing neuron firing
MOA of benzodiazepines
Think: FREnzodiazepine = increased FREquency
Facilitate GABA action by increased frequency of Cl channel opening
What is the treatment for status eplipeticus
1) Lorazepam (BZD)
2) Phenytoin (Na channel blocker)
3) Phenobarbital (if still seizing)