Flashcards in Pharm Deck (91):
What DA pathway controls movement?
What DA pathway controls reward and perception?
What DA pathway controls executive function?
What DA pathway controls pituitary prolaction function?
2 Post-synaptic enzymes that terminate DA action:
MAO A or B
Hyperfunctioning Migrostriatal pathway causes:
Hyper: dyskinetic movemnt
Hypo: dyskinetic movement, parkinsonism
Hyperfunctioning Mesolimbic pathway causes:
Hyper: Addiction, hallucinations
Hypo: amotivation, apathy
Hyperfunctioning Mesocortical pathway causes:
Hyperfunctioning Tuberoinfundibular pathway causes:
What drugs to enhance DA synthesis?
Levodopa: DA precursor
Carbidopa: combined therapy to prevent peripheral DA activity --> lower side effects
Results of low and high DA activity:
ADHD: ___ DA activity at ___
low, anterior cingulate
Parkinson: ___ DA activity at ___
Why is MTHFR enzyme important?
Creates L-methylfolate, which is the form that can cross BBB
TT alleles bad --> less DA made
Affects what pathway?
-Increase VMAT2 -->more DA release
2 wakefulness promoting stimulant drugs:
-Off label: ADHD
low dose is used for for?
high dose is used for?
Low dose: MAO-B selective --> Parkinson
High dose: MAO A and B --> Depression
MAOIs for Depression:
-MAOI decrease Serotonin breakdown
-Adding Serotonin drug --> toxic levels in CNS
-Tremor, muscle spasm, vital changes, hyperthermia, delirium, coma, death
effect on neurotransmitters?
-elevate DA and NE
D2 receptor agonists:
-Bromocriptine, pramipexole, ropinerole, Apomorphine injection
-Parkinson's or Restless leg Syndrome
D3 receptor agonists:
-Antipsychotic for Schizo
-Release DA, block DAT, stimulate D2
HTN, Schizo psychosis, causes Depression
Huntington's Chorea by lowering DA availability
D2 receptor antagonist affects which pathways?
ALL; they are non-selective
FGAs (high, low potency), SGAs
What causes EPS?
-High Potency FGA
-Akathisia, Dystonia, Parkinsonism, Neuroleptic Malignant Syndrome
Symptoms of Neuroleptic Malignant Syndrome:
2. Muscle rigidity
3. Vital sign instability
What is Tardive Dyskinesia
-Chronic D2 receptor antagonism
-Permanent movement disorder side effect
-Choreic or Athetotic movements
High vs Low Potency FGA drugs:
Blocking ___ receptor lowers EPS risk
Serotonin 2a (5HT2a)
Side effects of 'Dones' vs 'Pines'
Dones: more EPS
Pines: more sedating, more metabolic syndrome
Clozapine risks and benefits
-Risk of agranulocytosis
-Most metabolic risk of any agent
-No neuromuscular effect --> no EPS/TD
Blocking what receptor stops psychosis?
Mechanism of action for Beta blockers in Glaucoma?
Reduce aqueous production
Suffix for carbonic anhydrase inhibitors:
Mechanism of action for Carbonic Anhydrase Inhibitors in Glaucoma?
Reduce production of aqueous
Mechanism of action for Prostaglandin Analog in Glaucoma?
Increase uveoscleral outflow w/o effect on aqueous flow or trabecular outflow facility
Cocaine mechanism for diagnosing Horner's Syndrome
-Cocaine = reuptake inhibitor --> NE flood --> pupillary dilation
-Horner's Syndrome = dysfunctional PANS --> no pupillary dilation
What drug is used to differentiate preganglionic from postganglionic lesions in Horner's Syndrome?
Hydroxyamphetamine: Releases NE
Hydroxyamphetamine mechanism for differentiating lesion location in Horner's Syndrome
-No pupillary dilation = 3rd order neuron problem = Postganglionic = benign process
-Dilation = Preganglionic lesion --> requires investigation
How do you differentiate Adie's syndrome from an intracranial aneurysm?
-Low dose muscarinic agonist (Methacholine or Pilocarpine)
-Chronic denervated nerve in Adie's syndrom will be hypersensitive --> pupillary constriction
-Acute trauma neurved from aneurysm will not respond
What is light-near dissociation?
No pupil response to light, but does have accomodation
Most common cause and population affected by Parinaud's Syndrome
-Midbrain tumor (pineal)
Common presentation and population affected by Adie's Syndrome
-Loss of patellar reflex
What characterizes Argyll-Robertson Syndrome:
-Miotic irregular pupils
-Does not respond to cycloplegics
Triptan's mechanism of action:
5HT1 B-D agonist --> vasoconstriction of intracranial EXTRACEREBRAL blood vessels (trigeminovascular system) --> block sterile inflammation reaction
In what patient population are triptans contraindicated?
Patients w/ vascular disease, uncontrolled HTN, and comlicated migraine syndromes
Migraine vs Tension vs Cluster Headache characteristics:
Migraine: unilateral, throbbing, moderate-severe, aggravated by activity, relieved by rest
Tension: dull, achy, non-pulsatile, pressure-like, bilateral, mild-medium
Cluster: severe, unilateral, in temporal, orbital or supraorbital areas
Most commonly used Beta blocker for Migraine?
Most commonly used Ca++ Channel Blocker for Migraine?
-useful for aura
For what patient population is Migraine prevantative therapy recommended?
-3+ severe headaches/month or
-2+ mild-moderate headaches/week or
-inability to use effective symptomatic therapy
2 Anti-epileptics used for migraine prevention
Valproic Acid, Topiramate
Cluster Headache characteristics:
-Clockwork daily and annual rhythm (same time)
- Men:women 4:1
-Some patients have heavy facial features
Long-term Cluster Headache prevention drugs:
-Verapamil (Ca++ channel blocker)
-Valproic Acid (antiepileptic)
-Lithium (mood stabilizer)
Biogenic Amine Hypothesis of Depression:
Depression = too little CNS NE and/or 5HT
Scoring of Hamilton Depression Rating Scale (HDRS):
Very Severe= >23
What do MAO-A and -B mainly oxidize?
-A = NE, 5HT, Tyramine
-B = DA, phenyethylamine
What is the most used TCA for TTH prevention?
What is a common side effect of TCAs?
What 2 SSRIs have P450 Inhibition
What is Ketamine's mechanism of action?
Glutamate NMDA receptor antagonist
What drug can quitting smokers use to maintain nicotine abstinence?
Bupropion - Atypical antidepressant
What is the important side effect of Buproprion?
Lowers seizure threshold
What can happen if you give a Bipolar person tricyclics?
What are the 3 structural parts of local anesthetics?
1. Aromatic ring
2. Intermediate Linkage
3. Terminal Amine
If there is a big difference between pKa of local anesthetic and physiologic pH, what form will be more common? (uncharged/charged)
The (charged/uncharged) form of a local anesthetic can penetrate membranes
Which structural part of a local anesthetic determines lipid solubility and potency?
Metabolism of Ester vs Amide Local Anesthetics:
Esters: metabolized by plasma enzymes
Amides: Metabolized by hepatic P450 enzymes
How and where do local anesthetics bind intracellularly?
-Intracellular portion of Na channel
High risk for CNS toxicity from which 2 Local Anesthetics?
Which requires higher dose of Local Anesthetics: CNS or Cardio toxicity
What is Transient Neurological Syndrome and which local anesthetics can cause it?
-Severe transient pain from local anesthetic use in spinal anesthesia
-Lidocaine, Procain, Mepivacaine
Which group (ester or amide) of local anesthetics have high allergic reaction rates?
Esters -- PABA metabolites = known allergen
Which nerve fibers are first to be blocked by local anesthetics?
- B and A delta
-Generally: smaller, myelinated nerves blocked first
What are toxic side effects of Na+ channel blockers?
What is a side effect?
Toxicity = Dizzy, drunk, double vision
Side effect = 15% have rash, rare Steven Johnson syndrome
What is a contraindication for Valproate? Why?
Pregnancy -- 4-8% Teratogenic
What drugs can be given for status epilepticus?
IV: Phenytoin, Lorazepam, Diazepam, Valproate
What drug? Mechanism?
- T-type thalamus Ca++ channel blocker
Mechanisms for Anti-epileptics:
1. Voltage-gated Na+ channel blockers
2. Voltage-gated Ca++ channel blockers
3. Glutamate receptor blockers
4. GABA system agonists
Difference between Felbamate and Topiramate
Felbamate = NMDA blocker
Topiramate = AMPA and Kainate receptor blocker
Difference between toxicity and side effect
Toxicity: Unwanted effect of drug
Side effect: unexpected effect, not related to mechanism of action
Which anti-epileptic exhibits no metabolism?
What drug has synergistic action/competes with valproic acid
Antiepileptic drug with "word finding" problem toxicity
What is the Meyer-Overton Rule?
Potency of anesthetic gases directly related to their solubility in olive oil