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anxiety is an unpleasent state of tension, apprehension, or uneasiness that seems to arise from an unknown source.
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'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.
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?
what is GABA?
GABA is a neurotransmittor also known as y-aminobutyric acid and is the cheif inhibitory of the CNS
6 locations in the brain where you can find GABA receptors
1. cerebral cortex
3. basal ganglia
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?
This drug is a selective agoniist of the GABAa receptor, major psychoalkaloid present in many mushrooms
this drug acts like a non-competitive antagonists for the GABAa receptor chloride ion channels
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.
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
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
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?
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 within half-hr and lasts for about 6hrs
intermediate acting barbituates
what class of barbituates are used for daytime sedation and the treatment of seizure disorders and mild anxiety
long acting barbituates
which of the three important long acting barbituate drugs is unique due to its low lipid/water partition coefficient?
which of the three important long acting barbituate drugs is a long-actig sedative and hypnotic but also a valuble anticonvulsant?
which of the three important long acting barbituate drugs is used primarily for anticonvulsants and is considered a N-dealkylated phenobarbital?
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
one of the most active non-barbituate hypnotics that structurally stucturally similar and has the same toxic effects as barbituates.
Alcohols can also be used as a sedative and hypnotic. The order of potency of the alchols is the same as...
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
whats the Generic and brand of the drug that's officialy indicated as an antianxiety agent and also a sedative-hypnotic agent?
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?
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
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