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29 Cards in this Set
- Front
- Back
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What is tolerance?
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reduced drug effect with repeated use requiring a higher dose to produce the same effect
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What are the two types of tolerance?
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Pharmacokinetic
Physiologic |
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What is physiologic tolerance?
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Long term alterations at the primary synapses where the drug acts, as well as other synapses
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What is cross tolerance?
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tolerance to a drug in one class will usually produce tolerance to other drugs in the same class
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What is dependence?
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repeated compulsive use
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What is the difference between physiologic and psychologic dependence?
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Phsyiologic dependence forces use to avoid withdrawal
Psychologic dependence is a chase after rewarding effects and satisfy cravings. |
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What is cross dependence?
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Drugs from the same class can support individuals that are physically dependent on other drugs in that class.
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What is drug abuse?
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Repeated use of a drug that deviates from social norms and in disregard of harmful interpersonal or social consequences
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How do the capillaries in the brain differ from other tissues?
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Don't have fenestrations, have tight junctions instead which hinder the drugs and other material from the blood entering the brain.
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What two classes of drugs are used to slow the progression of Alzheimer's Disease?
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Cholinesterase inhibitors
NMDA receptor antagonists |
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What is the pathology of Alzheimer's Disease?
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loss of hippocampal pyramidal neurons and basal forebrain cholinergic neurons, causing impaired memory and cognitive ability.
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Name the cholinesterase inhibitors used to treat AD? How effective are they?
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Donepezil
Rivastigmine Galantamine Good for modest, temporary benefit |
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What are the NMDA receptor antagonist used to treat AD?
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Memantine
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What would be the benefit of using an anti-amyloid to treat AD?
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To stop the formation of A-beta amyloid plaques in the brain
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What would be the benefit of using ampakines to treat AD?
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AMPA receptor agonists
AMPA receptors mediate the majority of excitatory synapses and agonists could increase memory encoding |
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Discuss Donepezil: Disease treated, mechanism, major side effect.
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Alzheimer's
Cholinesterase inhibitor Mainly GI side effects |
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Discuss Rivastigmine: Disease treated, mechanism, major side effect.
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Alzheimer's
Cholinesterase inhibitor GI side effects with anorexia |
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What is the difference between donepezil and rivastigmine? (4)
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1. rivastigmine has butyrylcholinesterase blocking activity as well
2. and has non-hepatic (renal) clearance. 3. rivastigmine is available as a patch 4. more severe GI side effects |
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What is the difference between galantamine and donepezil?
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Galantamine can also allosterically modulate nACh receptors and enhance ACh release from the presynaptic terminal into the cleft.
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Discuss Memantine: Disease treated, mechanism, major side effect.
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Alzheimer's
Low affinity NMDA blocker GI side effects |
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What is the difference between memantine and phencyclidine or ketamine?
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PCP/ketamine (high affinity NMDA blockers) are non-selective NMDA blockers. Memantine (low affinity) shows selectivity to block only pathologic NMDA receptors.
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What the pathology of ALS?
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Degeneration of spinal, bulbar and cortical motor neurons causing muscle weakness and atrophy.
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Discuss Riluzole: Disease treated, mechanism (3).
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ALS
Inhibits glutamate release, blocks NMDA and kainate glutamate receptors, inhibits voltage-dependent Na channels. |
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Discuss Baclofen: Disease treated, mechanism.
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ALS
GABA(b) receptor agonist given intrathecal for spasticity |
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Discuss Tizanidine: Disease treated, mechanism.
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ALS
Alpha-2 agonist taken orally to manage spasticity |
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What drugs are used to manage ALS?
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Riluzole
Baclofen Tizanidine |
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What is the general pathology causing Huntington's and Parkinson's?
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Loss of neurons from the basal ganglia causing abnormalities in the control of movements
HD: htt mutation. Fragments of protein are deposited. PD: degeration of dopamine pathway from substantia nigra to striatum (nigral-striatal tract). |
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Discuss Tetrabenazine: Disease treated, mechanism.
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HD-Only FDA approved drug
Dopamine depleting: Inhibits VMAT2, blocking the uptake of dopamine into synaptic vesicles |
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What is the therapeutic strategy to treat PD?
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Increase dopamine levels in the striatum
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