Term
|
Definition
| hyperresponsivity, mast cell degranulation, inflammation |
|
|
Term
| First line reversal agents for asthma and COPD fall into these drug classes which act as sympathomimetics |
|
Definition
| Beta2agonists, nonselective beta agonists, direct and indirect acting sympathomimetics |
|
|
Term
| Examples of Beta 2 agonists (sympathomimetics) for asthma are: |
|
Definition
albuterol and levalbuterol (short acting)
salmeterol and formoterol (long acting) |
|
|
Term
| Examples of direct and indirect acting sympathomimetics for asthma treatment: |
|
Definition
|
|
Term
| Examples of nonselective beta agonist for asthma |
|
Definition
| isoproterenol, epinephrine/adrenaline |
|
|
Term
| Examples of methylxanthines for asthma tx: |
|
Definition
|
|
Term
| Mechanism of theophylline, a methlyxantine for asthma tx: |
|
Definition
| phosphodiesterase inhibitor; adenosine (A1) receptor antagonist |
|
|
Term
| Examples of PDE4 selective inhibitors in development for tx of asthma: |
|
Definition
| Roflumilast; Cilomilast/AIRFLO; tofimilast |
|
|
Term
| Second line muscarinic antagonists for tx of asthma: |
|
Definition
| ipratropium bromide, tiotropium bromide |
|
|
Term
| MOA of muscarinic antagonists for asthma tx: |
|
Definition
| blocks vaglly-induced bronchoconstriction |
|
|
Term
| MOA of inhaled corticosteroids for asthma tx (1st line therapy which can be used chronically): |
|
Definition
| anti-inflammatory (NOT bronchodilatory); decongestant-like activity in bronchi; potentialte beta2 actions to inhibit cytokine release. |
|
|
Term
| Examples of inhaled corticosteroids: |
|
Definition
| fluticasone and budesonide |
|
|
Term
| T/F long-acting beta2agonists MUST be combined with inhaled corticosteroids. |
|
Definition
| TRUE (serevent and foradil MUST have a corticosteroid like fluticasone or budesonide mixed in) |
|
|
Term
| MOA of Chromones for asthma tx (inhibition only agent, not for during an attack): |
|
Definition
| Alter chloride channel activity leading to inhibition of vagal activity, and eosinophil activation as well as mast cell degranulation . NO immediate effect on bronchial smooth muscle |
|
|
Term
| Examples of chromones for asthma tx: |
|
Definition
| cromolyn sodium, nedocromil (Tilade) |
|
|
Term
| 5-lipoxygenase inhibitor (a leukotriene pathway inhibitor) for asthma tx: |
|
Definition
|
|
Term
|
Definition
Prevents conversion of arachidonic acid into leukotrienes B4 (LTB4), and LTC4, and c LTD4
LTB4 can act as a chemoattractant for neutrophils > eosinophils via their actions on BLT receptors
Minor contributors to severity of asthmatic attacks
LTC4 and LTD4 (cysteinyl leukotrienes) can cause bronchoconstriction and inflammation via their actions on cysLT receptors |
|
|
Term
| Blocks aspirin-induces asthma: |
|
Definition
|
|
Term
| cysLT receptor antagonists (leukotriene pathway inhibitors) for asthma tx: |
|
Definition
| monteluast (singulair), zafirlukast (accolate)N |
|
|
Term
| MOA of IgE antibodies for asthma tx (3rd line): |
|
Definition
| Binds to IgE domain that binds to mast cells; Prevents the IgE from binding to and activating mast cells |
|
|
Term
| Examples of IgE antibodies for asthma tx: |
|
Definition
|
|
Term
Brand/genric for short acting beta2agonists:
ventolin/________ Xopenex/ _______ |
|
Definition
| albuterol and levalbuterol |
|
|
Term
brand/generic for non-selective beta agonist for asthma:
Isuprel/________ |
|
Definition
|
|
Term
Brand/generic for long-acting beta2agonists for asthma:
Serevent/______ Foradil/________ |
|
Definition
| salmeterol and formoterol |
|
|
Term
brand/generic for muscarinic antagonists for asthma:
Atrovent/____ Spiriva/_______ |
|
Definition
| ipratropium bromide and tiotropium bromide |
|
|
Term
brand/generic of inhaled corticosteroids for asthma:
Flovent/____ Pulmicort/_________ |
|
Definition
| fluticasone and budesonide |
|
|
Term
brand/generic for long-acting beta2agonists with corticosteroids added:
Advair/______ Symbicort/________ |
|
Definition
| salmeterol and fluticasone; formoterol and budesonide |
|
|
Term
| big categories of neurotransmitters: |
|
Definition
| amines and amino acids; peptides; gases; lipids |
|
|
Term
| MOA of botulinum toxin (botox) |
|
Definition
| inhibits release of neurotransmitters and smooths wrinkles or tx cerebral palsy |
|
|
Term
| ionotropic (fast) synaptic transmission is through: |
|
Definition
| excitatory (ligand- or voltage-gated ion channels like NMDA, AMPA, kainate) or inhibitory (ligand-gated ion channels) channels |
|
|
Term
| Metabotropic (slow) synaptic neurotransmission is usually through: |
|
Definition
| GPCRs (could be through ligand gating of voltage-dependent ion channels opened by G beta/gamma like K or Ca channels) |
|
|
Term
| groups of GPCRs (metabotropic [slow] gulaminergic neutrotransmitters): |
|
Definition
Group I: post-synaptic excitatory (mGlu1 and mGlu5)
Gq coupling PLC, IP3, DAG, intracellular Ca ++ release;
Group II pre-synaptic inhibitory
(mGlu2 and mGlu3) Gi coupling inhibition of cAMP inhibition of Ca++ channels; Group III: pre-synaptic inhibitory(mGlu4, 6, 7, 8)
Gi coupling inhibition of cAMP inhibition of Ca++ channels |
|
|
Term
| T/F GABA neurotrnasmission is INHIBITORY! |
|
Definition
|
|
Term
|
Definition
| inhibits VMAT and depletes dopamine stores |
|
|
Term
|
Definition
| increases dopamine release via the dopamine transporter |
|
|
Term
|
Definition
| partially selective D3 agonist |
|
|
Term
|
Definition
|
|
Term
|
Definition
| inhibits tyrosine hydroxylase and dopamine synthesis |
|
|
Term
| MOA for most antipsychotics: |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| antidepressants inhibiting the norepinephrine transporter |
|
|
Term
|
Definition
|
|
Term
|
Definition
| antidepressant inhibits MAOa |
|
|
Term
|
Definition
|
|
Term
| biosynthetic pathway of serotonin: |
|
Definition
| tryptophan to 5-hydroxytryptophan to serotonin to 5-HIAA |
|
|
Term
| MOA of many antipsychotics: |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
| inhibits tryptophan hydrolase and serotonin synthesis |
|
|
Term
| MOA of -triptans (antimigraine meds) |
|
Definition
|
|
Term
| What stimulates the syntehsis nad secretion of melatonin? |
|
Definition
| Beta 1 receptors on the pinealoytes (alpha 1 receptors help facilitate the response) |
|
|
Term
| melatonin receptor inhibited by melatonin: |
|
Definition
|
|
Term
| T/F botulinus and tetanus toxins inhibit ACh release, but black widow spider toxin stimulates release |
|
Definition
|
|
Term
| Murare and mecamylamine are antagonists at what receptor? |
|
Definition
|
|
Term
| order of increasing impact on CNS function of anxiolytics, hypnotics, neuroleptics, anesthetics, and euthanasia |
|
Definition
| Anxiolytic ~ Tranquilizer (Minor) ~ Sedative < Neuroleptic (Major Tranquilizer) < Hypnotic < Anesthetic < Euthanasia agent |
|
|
Term
| rolling stones song about sedative hypnotics: |
|
Definition
| mother's little helper (little yellow pill, probably valium/diazepam) |
|
|
Term
| Examples of some benzodiazepines: |
|
Definition
Chlordiazepoxide (LIBRIUM)
Diazepam (VALIUM)
Clorazepate (TRANXENE)
Oxazepam (SERAX)
Alprazolam (XANAX)
Estazolam (PROSOM)
Flurazepam (DALMANE) |
|
|
Term
|
Definition
|
|
Term
| Benzodiazepine Antagonist that can produce abstinence syndrome if patient has developed a physiological dependence: |
|
Definition
|
|
Term
| T/F The alpha1 subunit containing GABA receptors (BZ1 omega1 binding site) are associated with sedation and amnesia |
|
Definition
|
|
Term
| T/F Non alpha1 subunit containing GABA receptors (BZ2 omega2 binding site) may be associated with muscle relaxation and anxiolysis |
|
Definition
|
|
Term
| MOA of baclofen (lioresal) |
|
Definition
| an antispasmodic that is a GABAa agonist (coupled to Gi)which opens a K channel and hyperpolarizes cells |
|
|
Term
| MOA of gabapentin (neurontin): |
|
Definition
| used primarily as an antiepileptic drug not a GABA agonist may promote GABA release may help with spasms of Multiple Sclerosis |
|
|
Term
| Sedative hypnotic skeletal muscle relaxants for fibromyalgia or restless leg syndrome: |
|
Definition
pregabalin (lyrica)
also, the antidepressants amitriptyline (elavil) and fluoxetine (prozac) |
|
|
Term
|
Definition
Zolpidem (AMBIEN)
Zaleplon (SONATA)
Eszopiclone (LUNESTA)
Zopiclone (IMOVANE) Canada not US |
|
|
Term
|
Definition
| Bind to the benzodiazepine binding site of the GABA receptor; more selective than benzos by binding only to the alpha 1 and gamma 2 subunit (BD1 ω1 binding site) associated with sedation and amnesia |
|
|
Term
|
Definition
| Will compete with Z drugs for the BD1 omega1 binding site and counteract their effects |
|
|
Term
| Examples of barbiturates: |
|
Definition
| phenobarbital(nembutal), thiopental, |
|
|
Term
|
Definition
Rarely used as sedatives, bind to GABAa,
Still used as hypnotics e.g., thiopental and anticonvulsants, e.g., phenobarbital |
|
|
Term
| example of an Azaspirodecanediones which is used as a therapy for anxiety: |
|
Definition
| Buspirone (BUSPAR), a partial 5HT1A agonist with no GABAa interaction |
|
|
Term
| T/F Histamine acts on the NMDA receptor to enhance responses to glutamate |
|
Definition
|
|
Term
| T/F The first antipsychotic chlorpromazine is a derivative of the antihistamine promethazine |
|
Definition
|
|
Term
| T/F Beta blockers like propranolol can be used for performance anxiety |
|
Definition
|
|
Term
| Example of melatonin analog: |
|
Definition
| Ramelteon (ROZEREM) (don't use with cyp inhibitors or in hepaticcally impaired) |
|
|
Term
| T/F GABAA receptor is a major site of action of sedative-hypnotic drugs because they facilitate the inhibitory actions of GABA |
|
Definition
|
|
Term
| T/F benzo activity can be sustained for long durations via formation of active metabolites |
|
Definition
|
|
Term
T/F Tolerance to the therapeutic effects of Benzodiazepines can occur through
down regulation of BD binding sites |
|
Definition
|
|
Term
| song about alcohol by TOm T Hall, Garth brooks and george jones, and brad paisley: |
|
Definition
| I like beer, Beer Run, alcohol |
|
|
Term
| T/F 30% of hospital admissions are due in some way to alcohol |
|
Definition
|
|
Term
| what is the 2-step process that is the metabolism of ethanol? |
|
Definition
| ethanol is acted on by ADH to form acetaldehyde which is then aldehyde dehydrogenated to acetate |
|
|
Term
| T/F At high concentrations > 100 mg/dL or with chronic high consumption the mixed function oxidases of the liver will metabolize ethanol |
|
Definition
|
|
Term
| metabolism of ethanol follows what type of kinetics? |
|
Definition
|
|
Term
| MOA of acute ethanol consumption: |
|
Definition
| CNS effects caused by Potentiation of GABA at GABAA receptor to cause Mild euphoric state; Impairs NMDA receptor responses to glutamate and cause Blackouts; decreases catecholamines and decreases contractility in the heart; causes relaxation of muscles |
|
|
Term
| teratogenic effects of alcohol: |
|
Definition
Mental retardation
Intrauterine growth retardation
Movement disorders
Heart defects
Facial anomalies 1st trimester
Flattened features (thin upper lip) |
|
|
Term
| T/F you can decrease acute withdrawal symptoms from alcohol with benzodiazepines (diaxepam, lorazepam, oxazepam) or beta blockers like propranolol |
|
Definition
|
|
Term
| Opiod receptor antagonists that can eliminate the rewarding properties of ethanol: |
|
Definition
Naltrexone (REVIA)
Naltrexone (VIVITREX) |
|
|
Term
T/F Many asians have a
deficiency in Aldehyde
Dehydrogenase and have
reactions to ethanol as if
on disulfiram |
|
Definition
|
|
Term
| MOA of Acamprosate (CAMPRAL) for tx of alcohol dependency: |
|
Definition
Structural analog of GABA
May interact with both GABA and glutamate receptors
“restores the balance of excitatory and inhibitory neurotransmission”
Can be used with disulfiram
Can be used with naltrexone
Helps maintain abstinence
Does not seem to help
to initiate abstinence |
|
|
Term
| tx ethylene glycol (safe antifreeze) toxicity by: |
|
Definition
| Inhibit ADH to prevent formation of toxic metabolites with Fomepizole or Ethanol |
|
|
Term
| examples of injectable anesthetics: |
|
Definition
Barbiturates
Benzodiazepines
Propofol
Etomidate
Ketamine
Medetomidine and other alpha2 adrenergic agonists
Combinations (Neuroleptanalgesia, Conscious sedation ) |
|
|
Term
| Characteristics of injectable anesthetic agents: |
|
Definition
Rapid onset
Short acting
Used for induction prior to intubation for inhalation anesthesia
Fully efficacious
Often used in combination |
|
|
Term
| MOA of Thiopental (Pentothal, sodium Pentothal) |
|
Definition
| a barbiturate tat binds to the GABAa receptor and is an injectable anesthetic |
|
|
Term
| MOA of Midazolam (VERSED): |
|
Definition
| benzodiazepine IV product used as a pre-operative anesthetic/anxiolytic, binds to GABAa |
|
|
Term
| MOA of Propofol (DIPRIVAN), an injectable anesthetic |
|
Definition
Acts on GABAA receptor:
Prolongs channel open time
Can be agonist on its own
causes "less barfing" |
|
|
Term
| MOA of Ketamine (KETALAR) (IV) dissaciative anesthetic: |
|
Definition
NMDA receptor antagonist
Acts at PCP binding site psychotomimetic
Also subject to abuse
Special K, vitamin K, Kit-Kat
Bumpy re-emergence
Other sites of action
Nicotinic receptor
DO NOT USE WITH HEAD TRAUMA |
|
|
Term
| MOA of Medetomidine (DOMITOR) an injetable anesthetic agent" |
|
Definition
alpha2 adrenergic agonists IM, SC or IV
; Inhibits locus coeruleus; Analgesic actions at the level of the spinal cord; reversed by Atipamezole (ANTISEDAN)
Yohimbine (YOBINE) |
|
|
Term
| what is Neuroleptanalgesia? |
|
Definition
| a state of quiescence, altered awareness, and analgesia produced by a combination of an opioid analgesic and a neuroleptic. |
|
|
Term
| gas anesthesia was discovered by _________after he observed ether frolics |
|
Definition
|
|
Term
| Examples of gaseous anesthetics: |
|
Definition
| Ether (is explosive); nitrous oxide (MAC over 100%); Halothane (liver tox); Fluranes |
|
|
Term
| Goals of local anesthetics |
|
Definition
| block pain transmission, fast onset of action, long duration |
|
|
Term
| MOA of local anesthetics: |
|
Definition
block electrical conduction of nerve impulses along axons.
Dependent on voltage-gated sodium channels (NaV); Depolarization of adjacent membrane causes opening of the sodium channel; Action potential is sustained along the length of the axon |
|
|
Term
| T/F C fibers are smaller than Adelta fibers and easier to block |
|
Definition
|
|
Term
T/F Local anesthetics bind to the inside of sodium channels
They must cross the neuronal membrane as uncharged lipophilic molecules
Once inside neurons they become charged (ion-trapping) at intracellular pH |
|
Definition
|
|
Term
| T/F when giving local anesthetics, you can add sodium bicarbonate to alkalinize area to increase the proportion of uncharged state of the local anesthetic to increase the rate at which it penetrates the nerves. |
|
Definition
|
|
Term
| severe seizures due to local anesthetics can be treated with: |
|
Definition
|
|
Term
| T/F Many local anesthetics are sodium channel blockers, and as such are Class I antiarrhythmics and can be arrhythmogenic in a normally beating heart. |
|
Definition
|
|
Term
| Types of anti-seizure drugs: |
|
Definition
Sodium channel blockers
GABAA receptor facilitators
Glutamate receptor antagonists
Some also block calcium channels |
|
|
Term
| types of convulsant drugs: |
|
Definition
GABAA receptor inhibitors
Glycine antagonists
Sodium channel facilitators
Local anesthetics |
|
|
Term
| benzodiazepines for acute status epilepticus |
|
Definition
| diazepam (valium), clonazepam (klonopin), chlorazepate (tranxene), lorazepam (ativan) |
|
|
Term
| phenobarbital (nembutal) is a barbiturate that treats: |
|
Definition
| chronic seizures and acute emergencies |
|
|
Term
|
Definition
| a precursor or phenobarbital that is an anticonvulsant with a high incidence of hepatotoxicity and has active metabolites |
|
|
Term
| T/F you can use barbiturates in people with hepatic impairment |
|
Definition
|
|
Term
| examples of bromide anticonvulsants |
|
Definition
| potassium bromide, sodium bromide (both used in animals) MOA: mimic chloride ions and cause hyperpolarization in cells |
|
|
Term
| Hydantoins are use-dependent sodium channel (NAv) blocking antiseizure medications that treat: |
|
Definition
| generalized seizures (tonic-clonic) and partial seizures; ex. Phenytoin (dilantin |
|
|
Term
| examples of hydantoin anti-seizure medications: |
|
Definition
| phenytoin, mephenytoin, and fosphenytoin (prodrug) |
|
|
Term
| MOA of carbamazepine (tegretol) |
|
Definition
| use-depenent sodium channel blocker that is an anticonvulsant and also tx for bipolar disorder |
|
|
Term
| Oxcarbazepine (trileptal) is an anticonvulsant that works by: |
|
Definition
| prodrug with active metabolites that causes sodium channel blockade |
|
|
Term
| MOA of the anticonvulsant Vigabatrin |
|
Definition
| Gaba-T inhibitor, blocks coversion of GABA to glutamate |
|
|
Term
| Lamotrigine (Lamictal) MOA |
|
Definition
| Na channel blocker for partial seizures or bipolar disorder |
|
|
Term
| MOA of Gabapentin (neurontin) |
|
Definition
| gaba analog that may increase gaba release and is Cav antagonist |
|
|
Term
|
Definition
| tx partial seixures, inhibits synaptic release of gutamate, causes synaptic release of GABA, inhibits Cav |
|
|
Term
|
Definition
| blocks NAv and CAv, allosteric modulator of GABAa, inhibits Kainic acid receptor subtype of glutamate receptors, tx partial/generalized seizures and migraine |
|
|
Term
|
Definition
| Nav blocker, sulfonamide, partial/general seizures |
|
|
Term
|
Definition
| tx petit mal seizures; inhibits t-type Cav channels, targets thalamic neurons |
|
|
Term
| Valproic acid, sodium valproate (DEPAKENE) |
|
Definition
Treatment of absence seizures >> partial seizures
Treatment of infantile spasms
NaV blockade prolongs inactivated state
NMDA receptor blockade
GAD activator
More GABA synthesis
Inhibition of GAT-1
Inhibition of GABA-T
High concentrations only
Idiosyncratic liver toxicity – monitor liver enzymes!
Also used for bipolar disorder and migraine prevention |
|
|
Term
|
Definition
| tx absence seizures, inhibits t-type Cav |
|
|
Term
| schizophrenia is most often treated with |
|
Definition
|
|
Term
| three classical types of antipsychotics that are major tranquilizers/neuroleptics |
|
Definition
Phenothiazines chlorpromazine THORAZINE
Butyrophenones haloperidol HALDOL
Thioxanthines thiothixene |
|
|
Term
| newer, atypical antipsychotic agents: |
|
Definition
Clozapine CLOZARIL
Olanzepine ZYPREXA bipolar too
Risperidone RISPERDAL
Quetiapine SEROQUEL
Ziprasidone ZELDOX
Aripiprazole ABILIFY |
|
|
Term
|
Definition
| Phenothiazines are D2 and D4 receptor antagonists. They block the effects of dopamine on this receptor in the brain. Phenothiazines also have moderate alpha1 adrenergic, 5HT2 serotonergic, muscarinic and H1 histamine receptor antagonistic properties |
|
|
Term
| T/F butyrophenones are more potent than phenothiazines as antipsychotics. |
|
Definition
|
|
Term
| examples of nutyrophenones (antipsychotics which are also anti-emetics) |
|
Definition
| haloperidol(haldol) and droperidol with fentanyl (innovar) |
|
|
Term
|
Definition
The butyrophenones are D2 (and D4 ?) receptor antagonists.
They also block the effects of dopamine on this receptor in the brain.
Also have moderate 5HT2 serotonin, and alpha-1 adrenergic receptor antagonistic properties. |
|
|
Term
|
Definition
| cause motor disturbances, parkinson's-like disease, tardive dyskinesia, increase prolactin, causes hypotension |
|
|
Term
| droperidol and fentanyl (innovar) drug classes |
|
Definition
| a neuroleptic with an opiod agonist |
|
|
Term
| T/F At high doses neuroleptics produce catalepsy, which may be part of the reason that neuroleptanalgesia works so well for surgery |
|
Definition
|
|
Term
| Clozapine, an atypical antipsychotic, works by |
|
Definition
| binding to D4 receptor, very potent anti-psychotic, but it causes agranulocytosis |
|
|
Term
| Olanzapine (zyprexa) is an atypical antipsychotic and: |
|
Definition
| has a benzodiazepine nucleus, is associated with severe weight gain and dyslipidemia and may cause T2 DM |
|
|
Term
| atypical antipsychotics often target |
|
Definition
| dopamine receptors or 5HT2a receptors |
|
|
Term
| Propensity of newer anti-psychotics to cause diabetes mellitus: |
|
Definition
| Olanzepine >> risperidone ~ quietipine ~ clozapine > ziprasidone ~ aripiprazole ~ haloperidol |
|
|
Term
| T/F Aripiprazole may work in Alzheimer’s patients who have delusions and hallucinations |
|
Definition
|
|
Term
| T/F Long-acting injectable risperidone may be best for minimizing impairment of cognitive function |
|
Definition
|
|
Term
| T/F Paliperidone (a metabolite of risperidone) has no antagonistic activity at cholinergic receptors, it has low potential for anticholinergic adverse effects, including cognitive dysfunction |
|
Definition
|
|
Term
| new drug being developed for L-dopa-induced psychosis |
|
Definition
| Pimavanserin, an inverse agonist of 5HT2a |
|
|
Term
| MOA of lithium as an anti-manic |
|
Definition
| substitutes for sodium in cells and inhibits PLC pathway |
|
|
Term
|
Definition
CB-1 brain GPCR GI linked most in brain
Presynaptic inhibits GABA and glutamate release |
|
|
Term
|
Definition
| sodium channel antagonist broad range of efficacy |
|
|
Term
|
Definition
| first line for absence seizures |
|
|
Term
|
Definition
|
|
Term
| parkinson's can be caused by: |
|
Definition
| env. factors like rotenone, tricloroethylene, manganese; illicit drugs like MPTP; licit drugs like reserpine and antipsychotics |
|
|
Term
|
Definition
| NMDA antagonism and inhibits MAO reuptake |
|
|
Term
| Pentazocine (Talwin) is an opiod analgesic that: |
|
Definition
| is a kappa selective agonist and causes dysphoria |
|
|
