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47 Cards in this Set
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- Back
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Physostigmine: Mech Mode
Therapeutic use:
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reversible inhibition of cholesterase (i.e. an enzyme)
Muscular contraction and tonicity
Used to relieve intraocular pressure > glaucoma |
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Neostigmine Difference from Physostigmine |
ROA: Can be safely orally ingested |
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Rivastigmine: Difference from Physostigmine |
Can be applied through a patch - transdermal |
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Curare
Mech Mode
Site of action Therapeutic use: |
Antagonizes nACh receptor
Paralysis > can be fatal
NMJ in PNS
Adjuvant in surgical anaesthesia |
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Botox
Mech Mode |
Prevent vesicular release of ACh (interfers with vesicular fusion)
Paralysis of wrinkles/prevents contraction of sweat glands (also, asissts with migraines - look up how) |
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Parathion and Malathion What are they mostly used for Mech of action |
Pesticides/insecticides
Irreversible ACHe inhibitors |
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Barbiturates
Mech Mode Site of action.
Salient feature about Phenobarbitual |
Modulates activation and also activates GABA (A) receptors (No cap on the depressive continuum) Mode: Depress motor cognitive and behavioural functioning All through CNS but notably in brainstem
Half life = 120 hours
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Meprobamate (Miltown): What is it classified as? Marketed towards (3 groups) |
CNS depressant
Women, pregnant women and children |
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Qaaludes: Classified as...
Popularized as... |
Non-barbituate sedatives
Hallucinogens and aphrodisiacs (stimulates love feelings) |
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Valium Classified as... Mech Mode t(1/2) |
Benzodiazepenes
Facilitates opening GABA(A) (can't open by itself) Depress motor, cognitive and behavioural functioning t (1/2) = 24 hours |
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Ativan (Lorazepam) Classified as... Mech Mode t(1/2) |
Benzodiazepenes
Facilitates opening GABA(A) (can't open by itself) Depress motor, cognitive and behavioural functioning 15 hours |
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Halcion (Triazolam) Classifed as... Mech Mode t(1/2) |
Benzodiazepenes
Facilitates opening GABA(A) (can't open by itself) Depress motor, cognitive and behavioural functioning 2.5 hours |
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Zolpidem (Ambien), Zaleplon (Sonata), Eszopiclone (Lunesta)
What are they classed as? Mech Mode of action? |
Second generation/hypnotics Facilitates activity of the GABA (A1) receptor (A or A1? A1 may be a typo...)
Mode of action: hypnotics > induce sleep
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GHB: Mech. (generalised) Known for...
Popularized as (3 things) |
Potent CNS depressant Sedative date rape drug 1. General party drug 2. Body building aid 3. Sexual enhancement |
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Propofol Classed as... Mech Therapeutic uses |
Non-barbiturate sedative GABA (A) agonist
Surgical sedation/anaesthesia |
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Cocaine
Mech Mode ROAs (4) Sites of action: |
Mech: Antagonist for DAT Mode: 1. local anaesthetic 2. Vasoconstrictor 3. Psychostimulant
ROAs: Chewing (Coca leaf), Intranasal, Intravenous, Inhalation (Crack)
Mesolimbic, nigrostriatal p/ways and dopaminergic reward pathways |
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Amphetamines: General mech Modes Site of action
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Promotes release of NE and DA
1. Sympathomimetic 2. Vasoconstrictor effects 3. Psychostimulant
Mesolimbic pathway (higher doses = activation in Nigrastriatal p/way) |
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Methylphenidate (Ritalin) Mech.
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inhibits DAT; may slightly increase DA and NE |
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Caffeine Classified as... Mech Mode |
Purinergic Stimulant Antagonists of the adenosine receptor (Therefore stops release of GABA)
1. Vasoconstrictor 2. Psychostimulant
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Alcohol Mech Mode ~one drink dosage |
Mech: agonist of GABA(A); NMDA antagonist (which inhibits glu)
Mode: Dose dependent continuum B. disinhibition > Altered perceptions > alt. equilibrium > CNS dep. > Resp. dep., death
14 grams |
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Morphine Mech: Mode: |
Mech: opioid receptor agonist Mode: 1. To alleviate pain 2. To induce contented euphoria 3. Sedation |
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Codeine Mech Mode:
Salient feature of codeine |
Mech: opioid receptor agonist Mode: 1. To alleviate pain 2. to induce contented euphoria 3. Sedation
Pro drug: requires CYP2D6 to metabolise codeine into morphine |
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Oxycodone/ Hydrocodone Mech: Mode: |
Mode: 1. alleviate pain; 2. to induce contented euphoria; 3. Sedation
(Therapeutically used primarily as Analgesic ) |
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Heroin Mech: Mode:
Synthetic relation to morphine is... |
Opioid receptor agonist
1. alleviate pain; 2 induce contented euphporia; 3. sedation
A simple change; morphine + diacetylmorphine |
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Naltrexone Mech: Mode: |
Opioid receptor antagonist
No mode (?) > maybe the absence of effect |
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Methadone: Mech: Mode: t(1/2) Therapeutic aim: |
Long acting opioid receptor agonist possibly mild opioid agonist effects 20-40 hours Therapeutic aim: harm reduction > reduce needle associated disease, eliminate illicit drug use and crime |
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DOPA: What is it derived from? What is the enzyme that catelyses the change? What is the enzyme that catelyzes change to DA? What is L-DOPA classed as? What is the problem of L-DOPA? How can it be solved |
Tyrosine Tyrosine hydroxylase AA decarboxylase AA decarboxylase Prodrug It is converted in the periphery > doesn't reach CNS Take with Carbidopa
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Carbidopa: Mech: |
inhibits peripheral AA decarboxylase |
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Bromocriptive: Mech:
Advantages of Bromo. in treatment of PD (2)
Disadvantages (2)
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Agonist of the DA receptor
Doesn't require functional neurons to convert L-DOPA to DA Acts longer > t(1/2) = 12-14 hours
Older agents are marginally effective Side effects (e.g. hallucinations)
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Selegiline Mech:
Therapeutic use: |
Inhibitor of MOA-B (specific enzyme that clears DA)
Used as 3rd treatment option for PD |
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Memantine Mech:
problem with using in treatment of AD |
NMDA antagonist
Inhibiting NMDA causes amnesia > this is was of the debilitating severe symptoms of AD - therefore, treatment effects is limited |
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Chlorpromazine & Haliperidol Classified as Mech: Mode (in therapeutic terms)
Differences between the two? (2 p.kinetic differences and 1 p.dynamic effect) |
Primarily antagonist for the D2 receptor (60-70% blocked) Antipsychotics Decrease positive symptoms and increase functioning when treating schizophrenia
H. has better absorption and distribution; more potent |
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Clozapine Mech Mode
Notable side effect |
Weak D1, D2, D4 antagonist, stronger 5-HT1C, 5-HT2 antagonist Decrease in positive and negative symptoms (ScZ)
Agranulocytosis (a toxic interaction where blood cells create toxic intermediatory) |
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Risperidol Mech: Mode:
P.dynamic difference with Clozapine |
Weak D2 antagonist, strong 5HT2 antagonist
Decrease positive and negative symptoms (ScZ)
More selective in terms of receptors that are antagonized |
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Aripiprazole (Abilify ) Mech: Mode:
Advantage over Clozapine & Risperidol? |
Mech: Partial agonist for D2 and 5HT1A Decrease positive and negative symptoms (ScZ)
Full antagonists of D2 causes side effects > Abilify stabilizes system at lower amount of functioning |
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Parnate, Nardil and Marplan Classified as... Mech: Mode:
Major Disadvantage |
MAOIs Binds non-selectively and irreversible to MAO Improves mood and activity levels
Severe Drug-drug interactions Food interaction (the cheese effect) |
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Trofanil, Tryptomer, and Aventyl Classified as... Mech: Mode: |
Tricyclic Antidepressants
Mech: Antagonizes NET and SERT receptors (also blocks histamine and mACH receptors) Mode: elevates mood and activity, increase appetite and sleep, reduce morbid preoccupations (in dep. patients) |
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Classic atypical Anti-depressants Maprotiline (iodiomil) Mech:
Disadvantage |
SNRI
Seizure risk |
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Classic atypical Anti-depressants Amoxapine (Ascendin): Mech:
Disadvantage |
SNRI - i.e. blocks NE
Fatality and Parkinsonian risk |
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Prozac, Paxil and Zoloft Classified as
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SSRIs - blocks SERT |
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Fluoxetine Prozac
Mech:
Features of mode of action: |
SSRI - blocks SERT
Prolonged duration of action Slow onset of action (4-6 weeks) |
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Bupropion Mech |
SDRI - Inhibits DAT |
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Lithium Mech: Feature of Mech of action: Mode:
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Not fully understood Doesn't appear to work at the synapse A mood stabilizer |
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Valproic acid (valproate) classified as... Mech: Mode
Concern: |
Neuromodulator prolongs Na+ channel inactivation state; inhibits GABA transporter and GABA transaminase (i.e. increases GABA through two dif ways)
Slows behaviour'
teratogenic potential (general problem for all n.modulators is excitotoxicity)
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Carbamazepine Classified as Mech: Mode: |
Neuromodulator Prolongs Na+ channel inactivation state; potentiates GABA Slows behaviour |
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Lamotrigine (Lamictal) Classified as... Mode
Advantages (2) |
Neuromodulator Reduces-gated Na+ channel inactivation state, notably the Glutamatergic neurons
Less cognitive dysfunction; less teratogenic potential |
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Symbyax: State combinationm of drugs (2) and their classification State mechs of action for both
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Olanzapine: Antipsychotic mech: antagonizes D2 and 5HT
Fluoxetine (Prozac): Anti-depressant mech: SSRI > inhibits SERT |
