Drugs Flashcards
Bromocriptine
Full agonist
D2 receptors
Antiparkinsonian
^9-THC
CB1 receptor
Full agonist
Morphine
Mue opiate receptor
Full agonist
Nicotine
Nicotinic AcH receptors
full agonist
Muscle contraction or twitching
Verenicline(chantix)
Causes smoking to have less effect acts on a nicotinic AcH receptor
Partial agonist
Haloperidol
D2 receptor
Competitive antagonist
Antipsychotic
Gi
Clozapine
Dopamine receptors
Competitive antagonist
Atypical antipsychotic
Reserpine
blocks DA storage and depletes DA
decreases 3-MT, but increases DOPAC & HVA
(VMAT-1&2)
tropolone
COMT inhibitor
phenelzine (Nardil)
MAO inhibitors
non-specific
Antidepressents
moclobemide
MAO-A
NE is a substrate for MAO-A
deprenyl
MAO-B (at low doses, tends to affect DA more; used as an antiparkinsonian drug)
Catacholamine RELEASING AGENTS (Calcium independent)
=d-amphetamine (Dexedrine)
=l-amphetamine (Benzedrine)
=methamphetamine (Methedrine, “meth”; “crank”); stimulate release of monoamines, act as major stimulants, used to treat ADHD, common recreational drug
Methylphenidate (Ritalin): stimulates catecholamine release, acts as major stimulant, used to treat ADHD
ropinirole
D2 agonist
Gi
Catacholamine UPTAKE INHIBITORS - blocking transporter levels of transmission is high (more transmitter in the synapse)
Amphetamine Cocaine Methylphenidate (Ritalin) GBR 12909 (DA) Bupropion (Welbutrin, Zyban) (DA/NE) Desipramine (NE) anti depressent DAT is dopamine transporter Sert for seratonin Nat norepinephrin
PCPA
inhibits TrypH, blocks 5-HT synthesis
Tryptophan
Precursor
Deprevation reduces 5-HT
Tetrabenazine
(VMAT-2; less effect on 5-HT)
Storage of monoamine depletion and blocking
Block vesicular storage of monoamines (VMAT inhibitors)
p-chloroamphetamine;
5-HT RELEASE
potent at release of 5HT
higher doses of other amphetamines also release 5-HT
Mianserin
5-HT2 family antagonist
Pimavanserin
5-HT2A inverse agonist
clozapine, risperidol
Atypical Antipsychotics: clozapine, risperidol and related drugs are antagonists or inverse agonists of 2A and/or 2C receptor subtypes; many hallucinogens (e.g. LSD) also bind to 2A
Seratonin
Fluoxetine (prozac)
5_HT uptake
Selective in terms to DA and Epi and Norepi
Cocaine
Inhibit CA uptake
Uptake of seratonin
Non selective
Amphetamine
Higher doses affect uptake of seratonin
AcH esterase inhibitors ( blocking enzymatic enzymes) elevating Ach levels aka anticholinesterases
Physostigmine
Tacrine (alzaheimrs )
Galantamine (alzheimers)
DFP (organophosphate) irreversable inhibitors. Toxicity in farmers insecticides
Sarin nerve gases irreversable binds covalntly
Hemicholinium-3
Block choline transporter
Less moves into the neuron and this reduces the synthesis of Ach
Scopolamine
Muscurinic antagonist
antiparkinsonian,
hallucinogenic (high doses)
Autonomicsystem
produce dry mouth and constipation, and dilate pupils.
Drugs that block muscarinic receptors
Atropine
Muscurinic Antagonist
antiparkinsonian,
hallucinogenic (high doses)
Drugs that block muscarinic receptors can produce dry mouth and constipation, and dilate pupils.
Muscurine
Muscurinic agonist
Pilocarpine
Muscurininc agonist
Mecamylamine
Nicotinic antagonist
Curare
Nicotinic antagonist
used for research; can be lethal, stops the action of the diaphragm muscle; was used in blow darts and arrows in South America
Olanzopine
Block muscurinic receptors
MK 801 (dizocilpine)
noncompetitive NMDA antagonist, neuroprotective
PCP (phencyclidine) and ketamine
un-competitive NMDA antagonists.
Propranolol (Inderal)
b adrenergic competitive antagonists
used to treat high blood pressure
strychnine
Competitive antagonist in glycin
Rat poisin
physostigmine, tacrine, galantamine
tacrine & galantamine used to treat Alzheimer’s disease
reversible anticholinesterases
Affect the metabolism of Ach
nsecticides such as DFP, and the nerve gas Sarin
irreversible anticholinesterases
Bitopertin
GLYT-1 inhibitor, was evaluated as an adjunct treatment for schizophrenia
Rapastinel
GLY is a “co-agonist” on the NMDA receptor
is a partial agonist of this site
istradefylline and preladenant
A2A antagonists such as istradefylline and preladenant have been evaluated in clinical trials as antiparkinsonian drugs; istradefylline is approved for use in Japan, recently approved in US
Caffeine and other methylxanthines
are non-selective adenosine antagonists.
THC, CP55940
CB1 Agonists:
CP is much more potent
Thc could be an anelgesic
AM4113;
rimonabant
CB1 Antagonists/inverse agonists
Rimonabat was studied as a food suppressent
Codeine
agonists of opiote receptors
heroin
semi-synthetic drug
Propoxyphene (Darvon) Meperidine (Demerol) Fentanyl (Sublimaze) mixed with heroin due to high potency and affinity Knee receptors Oxycodone (OxyContin)
Synthetic opiates (“opioids”): Anesthesia and surgery uses
Naloxone ( receptor)
Opiate receptor antagonist
Peptides
Oxytocin Vasopressin Cholecystokinin (CCK) Neuropeptide Y
Tachykinins (neurokinins) Substance P Kassinin Neurokinin A Eledoisin
methamphetamine
It not only blocks DAT, it is a substrate, transported into the terminal
• Once inside the terminal, it stimulates release of DA
• Inside the terminal, it also blocks VMAT-2; it also is a substrate, transported into the vesicles
• It also inhibits MAO
FG7142
(benzodiazepine site) has effects opposite to benzodiazepines; can be described as a negative allosteric modulator
Pimavanserin:
5-HT2A inverse agonist;
used to treat hallucinations in Parkinson’s disease patients
neostigmine,
AChesterase inhibitor, used to treat neuromuscular dysfunction
stimulants, cold medicines/diet pills (ephedrine, phenylpropanolamine) that act on NE
These drugs can increase heart rate & blood pressure, and produce other signs of sympathetic activation
anticholinesterases, muscarinic agonists
Drugs that Stimulate ACh transmission: stimulate parasympathetic activity
Can cause SLUD!!! Salivation Lacrimation Urination Defecation YUK!!!!!!!!!!!!!
tropicamide,
Antagonist of muscurinic
can produce dry mouth and constipation, and dilate pupils.
Drugs that block muscarinic receptors
Dialating pupils for opthamologist
