PHARMACOLOGY Flashcards
What drug class is cocaine?
a noradrenaline reuptake inhibitor/ sodium channel blocker
what is cocaine used for?
a local anesthetic. It is applied to certain areas of the body (for example, the nose, mouth, or throat) to cause loss of feeling or numbness.
what is cocaines mechanism of action?
Cocaine produces anaesthesia by inhibiting excitation of nerve endings. This is achieved by reversibly binding to and inactivating sodium channels, which are necessary for the depolarization of nerve cell membranes and subsequent propagation of impulses along the course of the nerve.
what causes cocaine to be addictive?
the increase in dopamine levels it causes by preventing re-uptake of dopamine into pre-synaptic neurones
why does cocaine cause vasoconstriction?
This is a result of its blockade of norepinephrine reuptake in the autonomic nervous system
what drug class is dexamphetamine?
Noradrenaline releaser
what are amphetamines?
CNS stimultants
what are dexamphetamine’s effects?
elevations of systolic and diastolic blood pressures and weak bronchodilator and respiratory stimulant action
what are dexamphetamines proposed mechanisms of action?
1) Stimulation of the release of norepinephrine from central adrenergic receptors.
2) At higher dosages, it causes dopamine release from the mesocorticolimbic system and the nigrostriatal systems by reversal of the monoamine transporters.
3) Act as a direct agonist on central 5-HT receptors
4) Inhibit monoamine oxidase (MAO).
5) In the periphery cause the release of noradrenaline by acting on the adrenergic nerve terminals and alpha- and beta-receptors.
what drug class is dopamine?
Dopamine receptor agonist
what does dopamine act as an agonist for in the brain?
D1, D2, D3, D4, D5
how does dopamine cause an increased heart rate and cardiac contractility?
Dopamine acts on beta-adrenoceptors indirectly by causing release of norepinephrine from storage sites in sympathetic nerve endings producing positive chronotropic and inotropic effects on the myocardium
what drug class is hemicholinium?
choline re-uptake inhibitor.
what drug class us fluoxetine?
a selective serotonin reuptake inhibitor
what is fluoxetine used to treat?
depression, bulimia nervosa, premenstrual dysphoric disorder, panic disorder and post-traumatic stress
what is fluoxetine’s mechanism of action?
Fluoxetine is metabolized to norfluoxetine. Its mechanism of action is the inhibition of the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT1A autoreceptors.
what drug class is imipramine?
a catecholamine uptake inhibitor
what is imipramine’s mechanism of action?
inhibiting the sodium-dependent serotonin transporter and sodium-dependent norepinephrine transporter preventing or reducing the reuptake of norepinephrine and serotonin by nerve cells. The slowing of the uptake of these neurotransmitters is thought to contribute to relieving symptoms of depression.
how can imipramine cause enhanced serotonergic transmission with chronic use?
causes down-regulation of cerebral cortical b-adrenergic receptors and sensitization of post-synaptic serotonergic receptors
how long does it take to see antidepressant effects of imipramine?
2-4 weeks, can be up to 8 weeks