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95 Cards in this Set
- Front
- Back
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What are "dirty drugs" considered to be?
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Drugs used for different medical indications.
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What are CNS depressing Agents?
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Sedatives and hypnotics "downers"
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What are sedatives used for?
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They decrease activity, moderate excitement and calm the patient.
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What do hypnotics cause and facilitate?
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Cause drowsiness and facilitate the onset and maintenance of sleep state.
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What kind of sleep does hypnotics create?
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Sleep that resembles natural sleep. (electoencephalographic characteristics)
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Hypnotics must allow the patients to be easily what?
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Aroused easily.
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What else are hypnotics used for?
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Anxiety disorders, seizure, muscle spams.
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What are the three categories of insomnia?
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Transient, Short Term and Long Term
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What is transient insomnia duration?
What is it caused by? What is it often responded to? What kind of duration should the dose be? |
Less than 3 day duration.
Caused by brief stressor. Often respond to non-Rx therapy. Should be low dose and short duration |
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Short-Term insomnia what duration?
What is it caused by? |
3 days to 3 weeks.
Caused by personal stressor. |
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What is duration on long term insomnia?
Caused by what? |
More than 3 weeks.
No specific stressor identified. |
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What did benzodiazepines replace? Why?
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Replaced barbiturates due to increased margin of safety vs barbiturates.
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What are benzodiazepines sedative-hypnotic properties?
What kind of potency? |
Sleep Induction.
High anxiolytic potency relative to CNS depression. |
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What is Anxiety?
What kind of activation is it? What are symptoms of anxiety? |
Unpleasant state of tension, apprehension and fear.
Sympathetic activation: Fight or flight. Tachycardia, sweating, trembling, palpitations. |
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What are anxiety disorders defined as?
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Pathological manifestation of normal fear response
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What are the most common mental disorders?
What % of the Us population suffers from it? |
Anxiety disorders.
16% |
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What are 5 Benzodiazepines therapeutic effects?
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Reduction of anxiety, sedative and hypnotic effects, anterograde amnesia(loss of the ability to create new memories after the event cause by amnesia) , anticovulsant, muscle relaxant.
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What are pk parameters of Benzos?
What percent are bound to plasma proteins? |
They are lipophilic, rapidly and completely absorbed with large Vd.
70-99% |
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What are most Benzos extensively metabolized by?
What impact the duration of action? |
CYP3A4 and 2C19
Active metabolites. |
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What is the mechanism of action? (Where do they bind?) (What are the 2 receptors?) (What do the subtypes depend on?)
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Bind to the unique binding sites on GABAA receptors. The receptors are BZ1 and BZ2. Subtypes depend on which which "alpha" subunit is site of binding .
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GABA is a major what?
What does GABA binding lead to? |
Major inhibitoy neurotransmitter in CNS.
GABA binding leads to opening of Cl- channel and increase Cl conductance. |
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What do Benzos increase? How?
What kind of Effector is Benzo. |
Increase the frequency of channel opening by GABA.
Positive Allosteric effector. |
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What will Benzo binding increase?
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Will increase affinity of receptor for GABA.
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What is tolerance?
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With repeated dosing over time, a drug loses its effectiveness and an increased dose is required to produce the same physiological response.
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When does Benzo Tolerance appear?
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After long term of treatment
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What is Physical Dependence?
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Complex and poorly understood set of changes in the homeostasis of an organism that causes a disturbance of the homeostatic set point of the organism if the drug is stopped. The individual requires continued administration of the drug to maintain normal function.
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What happen at abrupt cessation of treatment?
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Withdrawal symptoms.
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For benzos, withdrawal symptoms can mirror what?
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Reappearance of anxiety symptoms.
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What is addiction?
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Compulsive drug use; a cluster of symptoms indicating that the individual continues use of the substance despite significant substance-related problems.
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What is an example of Benzodiazepine antagonist?
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Flumazenil
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What is the receptor antagonist on benzodiazepine antagonist?
What kind of inhibitor is it? What binding site is it at? |
GABA receptor.
Competitive inhibitor at BZ binding site. |
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What can benzodiazepine antagonist be used for?
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Can be used to reverse benzo action and as antidote for benzo overdose.
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How can benzodiazepine antagonist be administered?
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IV admin
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What is the onset and duration of benzodiazepine?
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Onset is rapid (1-2 min) but short duration (t1/2 ≈ 1 hr)
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What are barbiturate effective for? What is a downside of them?
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Very effective for sedation. They have a narrow therapeutic index.
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What has been a leading cause of death from drug overdoses for decades?
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Barbiturate poisoning
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What are the effects of barbiturate poisoning?
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Severe depression of respiration + central cardiovascular depression → shock-like condition, coma
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What enzymes do barbiturates induce?
What are the side effects of barbiturates? |
Induce CYP P450.
Cause physical dependence, drug hangover and several withdrawal symptoms. |
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What do barbiturates depress?
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Reversibly depress the activity of all excitable tissues.
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What is CNS depression?
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mild sedation → general anesthesia.
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What is Respiratory Depression?
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suppress hypoxic and chemoreceptor response to CO2
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What is an overdose described as?
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respiratory depression and death
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What is sensitive to barbiturates?
Where are there direct effect? |
The CNS is exquisitely sensitive to barbiturates → direct effects on peripheral excitable tissues are weak.
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Where do serious in cardiovascular and other peripheral functions occur ?
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in acute barbiturate intoxication.
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What are the barbiturates receptors?
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GABAA receptors
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How are Barbiturates and Benzos related in MOA?
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Barbiturates, like benzos, enhance the binding of GABA to GABAA receptors, however, they promote (rather than displace) the binding of benzodiazepines
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How do barbiturates potentiate GABA-induced chloride currents?
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By prolonging the duration of channel opening occur rather than by increasing the frequency of these bursts (as benzodiazepines do)
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What can Barbiturates block?
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Can block excitatoy glutamate receptors.
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What is glutamate?
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Glutamate is a principle excitatory neurotransmitter.
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The GABAA Receptor is the hub for what?
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allosteric regulation by myriad drugs
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What are clonazepam and clorazepate used for?
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Chronic seizure Rx
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When Alprazolam is used for what?
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Panic disorder
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Lorazepam and Temazepam doesn't have what?
What does it decrease than increase? |
No phase 1 metabolism and decrease DDI and increase safety
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What may Benzos disturb?
What do benzos have potential for? |
Benzos may disturb intellectual function and motor dexterity.
Benzos have potential for dependence; withdrawal seizures |
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Barbiturates induce what?
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tolerance, drug metabolism enzymes and physical dependence.
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Zolpidem and Zaleplon are what kind of agonists?
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non-benzo BZ1 agonist
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Ethanol is what kind of depressant? what kind effects?
What does it have potential for? |
CNS depressant with sedative and anxxiolytic effects.
High tox potential |
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What do antihistamines block?
What do they inhibit the uptake of? |
Block histamine H1 receptors
Inhibit uptake of serotonin |
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What are antihistamines T1/2?
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9 hrs
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What are psychomotor stimulants? What do they increase and increase?
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Excitement and euphoria. , ↓ fatigue, ↑ motor activity
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What are examples of CNS stimulants?
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Caffeine, nicotine, varenicline, Cocaine and amphetamines
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What is the most highly consumed stimulant in the world?
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Caffeine
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Caffeine and theophylline are what group?
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methylxanthines
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What kind of receptor is involved with caffeine?
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Adenosine receptor competitive antagonist
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What receptor family is caffeine part of?
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GPCR; 4 subtypes. A1 (Gs coupled) and A2A (Gi coupled).
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Caffeine is involved in what processes?
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Nuerotransmitter release in the CNS, regulation of blood flow.
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At very high doses of caffeine there is translocation of what?
Inhibition of what? Which increases what? |
Translocation of extracellular Ca2+.
Inhibition of phosphodiesterases which leads to increase of cAMP and cGMP |
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What happens effects are present at 100-200 mg of caffeine.
What happens at higher doses? |
Decrease fatigue and increased alertness.
Anxiety and tremors |
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What is the active ingredient in tobacco?
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Nicotine
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What is the 2nd most widely used CNS stimulant and the 2nd most abused drug ?
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Nicotine
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What is nicotines addictive characteristics?
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physical dependence occurs rapidly and can be severe
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What is the MOA of Nicotine?
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alpha4β2 neuronal nicotinic acetylcholine receptor agonist
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What is varenicline used for?
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treatment for smoking cessation
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What is Varenicline MOA?
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alpha4β2 neuronal nicotinic acetylcholine receptor partial agonist
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What is useful for mgt of nicotine withdrawal symptoms.
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Varenicline
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What is an amphetamine? What kind of clinical effects?
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non-catecholaminergic sympathetic amine w/ clinical effects similar to cocaine
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What is Dextroamphetamine (DEXEDRINE) action?
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greater CNS action and fewer peripheral effects
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What is narcolepsy?
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Chronis sleep disorder where you fall asleep at inappropriate times)
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When do narcolepsy patients reach REM sleep compared to normal sleep?
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REM sleep w/in 10 min (vs. 90 min for normal sleep)
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What are effects of Narcolepsy?
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Cataplexy (loss of muscle function)
Sleep Paralysis Automatic behavior) |
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What do amphetamines stimulate?
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Stimulates entire cerebrospinal axis: cortex, brain stem, medulla
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What do amphetamines elevate?
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Elevation of catecholamine neurotransmitters in synaptic spaces
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What do amphetamines enhance the release of?
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Enhances release of dopamine, norepinephrine and serotonin
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What are amphetamine side effects?
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↑ alertness ↓ fatigue↓ appetite, insomnia
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In addition to CNS, what else do amphetamines act on?
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acts on adrenergic system via norepinephrine release (sympathetic nervous system)
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What are some cardiovascular effects?
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Cardiovascular effects: headache, chills, palpitations, cardiac arrhythmias, hypertension or hypotension, circulatory collapse
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What do amphetamines inhibit? What does this result in?
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Inhibits monoamine oxidase (degrades neurotransmitters)→ ↑ neurotransmitters in synaptic space
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What else do amphetamines inhibit?
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Inhibit monoamine neurotransmitter uptake by monoamine transporters
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What are the three main types of GABA Receptors?
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A, B, C
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The GABAa receptor is what kind of receptor?
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ligand-gated Cl- ionotropic receptor
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What agent does the GABAa receptor bind to?
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EtOH, benzos, barbituates
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What kind of receptor if the GABAb receptor?
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The GABAB receptor is a metabotropic receptor coupled to Gi
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What does the GABAb receptor active and reduce?
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Activate K+ channels and reduce Ca++ conductance
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How much energy is in a hydrogen bond?
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hydrogen bond is small, but collectively the hydrogen bonds can improve water solubility by interacting with water molecules and making the molecules more “hydrophilic” (“water loving”).
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What must nonprescription drug products have on them?
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Labeling
Product information Drug interactions Allergies Handling and storage |
