Term
phentermine
benzphetamine
diethylpropion
phendimetrazine |
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Definition
noradrenergic drugs for short term use as anorexants
enhance the action of NE in the CNS
closely related to amphetamine and methamphetamine |
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Term
1) phenethylamine would be expected to demonstrate little pharmacological activity due to rapid metabolism by MAO
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2) substitution on the alpha carbon increases CNS activity relative to peripheral effects and slows metabolism by MAO
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3) introduction of substituent on the alpha carbon introduces a chiral center. in the case of amphetamines, the S-isomer is 10-fold more potent than the R-isomer
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4) hydroxylation on the phenyl ring or beta carbon decreases CNS activity
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5) haloenation of the ring generally decreases activity at adrenergic receptors, but may enhance action at serotonin receptors
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6) in most cases, disubstitution on nitrogen eliminates direct receptor interaction. also these compounds usually produce less CNS stimulation than compounds with small monosubstitutions. many of these N,N-disubstituted products will maintain the anorexiant activity
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7) since many amphetamine-like compounds are related structurally to NE, it is not unexpected that they can affect neuronal processes. also, these compounds bear some structural resemblance to dopamine and serotonin. Thus, some of there actions may be related to other neurotransmitter systems
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Definition
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the resin containing the acidic sulonic acid group is prepared by forming the sodium salt with the strong base, NaOH. the drug, phenteramine in its protonated form, exchanges with the Na ion (cation exchange). as the resin passes through the intestine, it reaches equilibrium with high electrolyte concentration and releases the drug. |
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Definition
| MOA of phenteramine resin |
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Term
benzphetamine is metabolized to methamphetamine and amphetamine
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Definition
| why is the abuse potential for benzphetamine high? |
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Term
these compounds typically have a pKa of 9-9.5
increasing urine pH will decrease the elimination of amphetamine-like compounds
decreasing urine pH will increase the elimination of amphetamine-like compounds
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Definition
| pH effect on the elimination of amphetamine like compounds |
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Term
undergoes metabolism by CYP3A4 to 2 active metabolites
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Definition
metabolism of sibutramine (withdrawn)
reuptake inhibitor of NE, 5HT, and to a lesser extent dopamine |
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Term
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Definition
| this enzyme is specific for esters in the alpha position longer than 10 carbons long |
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Term
hydrogenated derivative from the naturally occuring product lipstatin
exerts its MOA through a 4 membered lactone (cyclic ester)
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attack of a key serine hydroxyl at the active site of pancreatic lipase on the lactone group of orlistat yields a covalent bond (ester) with the enzyme
this bond, though covalent, is not considered irreversible due to hydolysis of the ester linkage
more resistant to hydolysis than other esters b/c of steric hindrance of long chain on orlistat
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Definition
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Term
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Definition
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Term
anandamide - increased selectivity for CB1
arachidonoylglycerol
noladin ether - specific agonist at CB1 |
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Definition
| endogenous cannabinoid ligands that have been identified. |
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Term
| fatty acid amide hydrolase (FAAH) |
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Definition
| a key enzyme that is involved in the degradation of anandamide that may be a useful target for the development of therapeutic agents |
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Term
delta-9-THC
metabolite: 11-OH-delta-9-THC
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Definition
appetite stimulating effect attributed to agonist effect at CB1 receptor
active metabolite is more active than parent
psychoactive, hallucinogenic, euphoric, sedative, appetite stimulating effects |
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Term
rimonabant
taranabant
CNS side effects (anxiety/depression) due to stimulation of CB1 receptors in the CNS
design compounds with preference for peripheral CB1 receptors by increased total polar surface area and decreased log P
CNS CB1 blockade: decreased food intake, decreased body weight, no effect on insulin sensitivity
peripheral CB1 blockade: decreased food intake, decreased body weight, increased insulin sensitivity |
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Definition
CB1 receptor antagonists/inverse agonists
decrease food intake, decrease appetite |
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Term
ephedra, Ma Huang
FDA required the removal of all ephedra from dietary supplements |
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Definition
active ingredients are ephedra, ephedrine, and pseudoephedrine
both direct and indirect effects on adrenergic receptors
possibility of serious side effects
increases energy expenditure |
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Term
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Definition
used in the treatment of depression
role in 5HT - blocks reuptake
inducer of CYP3A4, possibility of serious drug-herbal interactions |
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Term
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Definition
catus used to prevent hunger and thirst during long hunting expeditions
steroid glycoside is the active ingredient
decreases appetite |
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Term
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Definition
active ingredient is cathinone a potent amphetamine like compound that is metabolized to cathine (norpseudoephedrine)
structural similarity to diethylpropion
increases energy expenditure |
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Term
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Definition
active ingredient: phenylalkylamines
causes increased energy expenditure
potential risk in patients with hypertension, tacharrhythmias |
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Term
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Definition
active ingredient: epigallocatechin gallate (EGCG) and caffeine
EGCG is an inhibitor of COMT leading to enhanced actions of NE
caffeine is a PDE inhibitor, increases cAMP and increases levels of hormone sensitive lipase and can stimulate lypolysis |
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Definition
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Term
| conjugated linoleic acids |
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Definition
| may decrease fat disposition in adipose tissue, may enhance fat oxidation, may inhibit lipoprotein lipase |
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Term
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Definition
active ingredient: hydroxycitrate
inhibits citrate lyase; thus, decreasing long chain fatty acid synthesis
may block 5HT and other NT reuptake |
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Term
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Definition
active ingredient: caffeine
increase energy expenditure |
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Term
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Definition
active ingredient: C30 compounds (saponins), glycosides
may decrease glucose, maltose, oleic acid absorption. decrease appetite |
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Term
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Definition
active ingredient: pregnane glycosides
appetite suppresant, blocks citrate lyase (thus decreasing fatty acid synthesis) |
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