MED.CHEM EXAM IV PACKET 3
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88 terms
Terms | Definitions |
|---|---|
 Therapeutic effect of Sedative Drugs? | Sedatives induce calm, without producing sleep |
| Therapeutic effects of hypnotic drugs? | Hypnotics induce sleep |
| What are Anxiolytic Drugs used for? | are used to treat symptoms of anxiety |
| define anxiety | anxiety is an unpleasent state of tension, apprehension, or uneasiness that seems to arise from an unknown source. |
| Symptoms of anxiety is said to be similar to those of what? | fear |
| Muscle relaxants are also known as? | -Neuromuscular blocking drugs -Spasmolytics |
| What are Muscle relaxants drugs? | muscle relaxants are drugs which affect skeletal muscle function and decrease muscle tone. |
| What are your anticonvulsant? | Diverse group of pharmaceutical used in treatment of epileptic seizures. Anticonvulsants are also increasingly being used in treatment of bipolar disorder. |
| Why are anticonvulsants used to treat bipolar disorders? | anticonvulsants used to treat bipolar disorders because they act as mood stabilizers |
| What are anesthetics? | Anesthetics are drugs that cause anesthesia |
| What is anesthesia? | Reversible loss of sensation. |
| What's the difference between the older Sedatives, Hypnotics, and Anxiolytics as compared to the newer ones | To get to a level of anesthesia with the older drugs you risked death but with newer ones you can increase the dose and never get too deep of an anesthetic effect that may risk coma or death. |
| What are the two classes for Sedative-Hypnotic Drugs? | 1. Barbiturates 2. Non-Barbiturates |
| Non=barbiturates class can be broken down into 5 more categories what are they | 1. Aldehydes and aldehyde derivatives 2. Piperidine derivatives 3. Quinazoline derivatives 4. Alcohols and their carbamate derivatives 5. Benzodiazepine derivatives |
| studies show that, the neuronal effects associated with anxiolytics, sedatives, and hypnotics effects, especially positive modulation of GABAa receptors also relate to what other effects? | anticonvulsant effects |
| What are the GABA receptors? | A class of receptors that respond to the neurotransmitter GABA |
| what is GABA? | GABA is a neurotransmittor also known as y-aminobutyric acid and is the cheif inhibitory of the CNS |
| What are the two classes of GABA | GABAa and GABAb |
| which class of GABA receptors are ligand gated chloride ion-channels | GABAa |
| which class of GABA receptors are protein-coupled receptors? | GABAb |
| 6 locations in the brain where you can find GABA receptors | 1. cerebral cortex 2. hippocampus 3. basal ganglia 4. thalamus 5. cerebellum 6. brainstem |
| most of the GABAa receptors consist of what comboniation of subunits? which are most common? | Alpha, Beta, and Gamma most common will be alpha-1, beta-2, gamma-2 |
| the active site of GABAa receptors are also the binding site of what three common drugs? | -Gaboxadol -Bicuculline -Muscimol |
| This drug is a selective agoniist of the GABAa receptor, major psychoalkaloid present in many mushrooms | Muscimol |
| This drug is an experimental sleep aid drug | Gaboxadol |
| This drug is light-sensitive competitive antagonist of GABAa receptors. | Bicuculline |
| This drug blocks the action the inhibitiory action of GABAa receptors | bicuculline |
| the action bicuculline mimics what condition? | epilepsy |
| this drug acts like a non-competitive antagonists for the GABAa receptor chloride ion channels | Picrotoxin |
| Picrotoxin is a channel blocker or a recptor antagonist? | channel blocker |
| infusion of picrotoxin has what type of effects? | 1. stimulant 2. convulsant. |
| the binding sites of GABAa receptor are also called? | Allosteric binding sites |
| What are barbiturates? | CNS depressants |
| What effects do barbiturates produce? and what exactly are they used for? | Barbiturates produce a wide spectrum of effects from mild sedative to coma. Barbiturates are used as sedatives, hypnotics, anesthetics, and anticonvulsants |
| Whats the issue with barbiturates? | they can e addictive and abused. Excessive use of barbiturates can caused depression, slurred speech, slowed reflexes and confusion. |
| bariturates can undergo what type of tautomerism? | keto-enol tautomerism |
| What's the benefits of Keto-enol tautomerism of barbituric | it allows the formation of water-soluble salts with a strong base since barbiturates are not readily dissolved in water |
| What two compounds help maintain the pH of barbiturates between 10 and 11? | Na2CO3 & CO2 |
| barbiturates should not be placed in acidic solutions or mixed with acidic solutions why? | because the barbiturates may percipatate as free acids |
| Barbiturates binds where to exer their characterstic CNS effects? | allosteric binding sites on GABAa receptors |
| Whats the effect of having barbiturates bind to allosteric binding site GABAa receptors? | 1. they can positively modulate the effects of the GABAa - GABA combinations 2. Can increase chloride ion influx by without GABA attaching to its receptor site on GABAa |
| What is the term associated with the effects barbiturates produce after binding to GABA receptors? | GABA mimetic effects |
| Barbiturates also block what receptors besides GABA? | AMPA |
| what is the principal excitatory neurotransmitter in the mammalian CNS? | Glutamate |
| what is AMPA receptor? where is its name derived from? | alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor - is a non-NMD-type ionotropic transmembrane receptor for glutamate. name derived from its ability to be activated by the artificial glutamte analog AMPA |
| SAR of barbiturate: Hypnotic activity | -side chains at position 5 -both hydrogens at position 5 must be replaced |
| SAR of barbiturate: Potency and DOA | Length of the side chain at position 5 influences potency and DOA. the bigger the side chain the more potent. |
| SAR of barbiturate: rapid onset /shorter DOA | sulfur instead of oxygen at position 2 has has more rapid onset of action but shorter DOA |
| SAR of barbiturate: increase in potency, rate of onset, and short action | -increase in lipophilicity -branched/cyclic/unsaturated side chain will decrease DOA |
| reviewing the hypnotic activity of barbiturates what if we failed to replace one of the hydrogen at position 5 of the barbiturate? | the barbiturate may succeptible to tautomerization to a highly acidic compound triihydroxypyrimidine |
| reviewing the SAR of barbiturates what simple factor will cause the barbiturate to become more hydrophilic? | by adding the polar groups to the alkyl sidechain at position 5 on the barbiturate structure |
| SAR of barbiturate: substitution on nitrogen | -substitution of one of the hydrogens on the imidie in the barbiturate by alkyl groups increases lipid solubility. -as the size of the N-alkyl group increases so does lipophilicity |
| reviewing the SAR of barbituates and the effects that can be produced after substituting one the hydrogens on the imide what can impart convulsant like properties to the barbituate? | -The attachment of large alkyl groups |
| SAR of barbiturate: moodifications what position(s) are of primary importance in the barbituates used as anticonvulsants and anesthetics? | N1 and N3 |
| What are 4 classes to classify barbituates? | 1. Ultra-short 2. Short-acting barbituates 3. intermediate acting barbituates 4. long-acting barbituates |
| what class of barbituates produce anesthesia within 1min after IV administration | ultra short acting barbituates |
| what class of barbituates produce action with half-hr and last about 4hrs | short-acting barbituates |
| what class of barbituates produce action within half-hr and lasts for about 6hrs | intermediate acting barbituates |
| what class of barbituates produce action within half-hr and lasts for 8hrs | long acting barbituates |
| what class of barbituates are used for daytime sedation and the treatment of seizure disorders and mild anxiety | long acting barbituates |
| name the three important long acting barbituate drugs | 1. barbital 2. phenobarbital 3. mephobarbital |
| which of the three important long acting barbituate drugs is unique due to its low lipid/water partition coefficient? | barbital |
| which of the three important long acting barbituate drugs is a long-actig sedative and hypnotic but also a valuble anticonvulsant? | phenobarbital |
| which of the three important long acting barbituate drugs is used primarily for anticonvulsants and is considered a N-dealkylated phenobarbital? | mephobarbital |
| which class of barbituates are used primarily as sedative-hypnotics | Intermediate Duration of Action |
| the two barbituate drugs you must remember for intermediate DOA | 1. amobarbital 2. butabarbital |
| the barbituates that have substituents in the 5 position proomoting more rapid metabolsim than the intermediate barbituates are known as | barbituates with a sort duration of action |
| the two important barbituate drugs with a sort duration of action are? | -secobarbital -pentobarbital |
| one of the most active non-barbituate hypnotics that structurally stucturally similar and has the same toxic effects as barbituates. | -Glutethimide (Doriden) |
| Alcohols can also be used as a sedative and hypnotic. The order of potency of the alchols is the same as... | marchovnikof rule: 3>2>1 |
| what happens when you replace the hydrogen atom in the alkyl group with an halogen of alcohols with barbituate activitiy | will increase potency |
| carbabmylation of alcohols generally produce what effect | generally increases the depressants potency |
| what is the Ethchlorvynol (Placidyl) ? | mild sedative-hypnotic with quick onset and short DOA |
| whats the Generic and brand of the drug that's officialy indicated as an antianxiety agent and also a sedative-hypnotic agent? | meprobamate |
| benzodiazepines binds to the interface of what subunits of the GABAa receptor ? | alpha and gamma subunits |
| which subunits are required for sedative and hypnotic effects and anticonvulsant effects of benzodiazepines? | alpha-1 subunits |
| which subunits are required for anxiolytic effects of benzodiazepines? | alpha-2 subunits |
| which subunits are involved in other miscellaneous actions of benzodiazepines? | alpha-3 and alpha-5 |
| which subunit is required for most positive allosteric effects? | gamma-2 subunit |
| most classical benzodiazepines are what type of modulators? | positve modulators |
| whats another name for the benzodiazepine recognition site? | allosteric site |
| what are known to be negative modulators at benzodiazepine modulatory site? | beta carbolines |
| antagonist, zero modulators, and neutralizing allosteric modulators are all defined as | compounds that can occupy benzodiazepine modulatory sites and have no effect on chloride flux themselves and can block positve as well as negative modulators. |
| SAR of Benzodiazepines: what is required for activity that may participate in pi-pi stacking with amino acid residues on the receptor | Aromatic or heteroaroomatic ring |
| SAR of Benzodiazepines: what is required for general activity and how can you increase the activity of benzodiazepines | -an electornegative substituent at position 7 is required for general activity - position 6 8 9 must be vacant -the more electronegative the substituent is at position 7 the higher the activity |
| SAR of Benzodiazepines: phenyl ring at position 5 promotes activity but how can u increase this activity? | if this pheny roup is positioned ortho (2) or diortho (2,6) substituted with EWG activity is increased. |
| SAR of Benzodiazepines: what is the importance of 2-carbonyl function and the nitrogen atom at positon 1 | important for benzodiazepine activity |
| 5 therapeutic uses of benzodiazepines | Panic disorders Generalized anxiety disorders insomnia seizures alcohol withdrawl |
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