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Block C > Flügge > Flashcards

Flügge Flashcards

1
Q

Pharmacokinetics

A

Fate of the drug in the organism

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2
Q

Pharmacodynamics

A

Physiological and biochemical interactions of drug and target tissue

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3
Q

Biological effects of free drugs and metabolites

A

Regulation of enzymes

Regulation of channels

Binding to receptors

Binding to transporters

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4
Q

Molecules passing walls of capillaries

A

Typical: small molecules by diffusion; small fenestrae for high volume passage

Brain: no intercellular clefts => hydrophilic molecules cannot pass; D-glucose and amino acids actively transported

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5
Q

Liposomes

A

Artificially prepared vesicles formed by a lipid bilayer

For application of nutrients or pharmaceutical drugs

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6
Q

Nanoparticles

A

Diameter 1 to 10,000 nm

May pass the ‘leaky’ blood vessels in a tumor for drug delivery

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7
Q

Choroid plexus

A

Produces cerebrospinal fluid

Epithelial cells forming a boundary that can be passed by some drugs

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8
Q

CSF

A

Cerebrospinal fluid

Produced by the choroid plexus

Fills subarachnoid space

Provides micronutrients, neurotrophins, hormones, etc

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9
Q

Drug metabolism: phase I

A

Cytochrome P 450 metabolises drugs making them less lipophilic

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10
Q

Drug metabolism: phase II

A

Conjugation with glucuronic acid making the drugs more hydrophilic

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11
Q

Factors influencing drug metabolism

A

Enzyme induction (used repeatedly?)

Enzyme inhibition (several drugs?)

Drug competition

Genetic polymorphisms

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12
Q

ED50

A

Effective dose

Concentration which leads to the desired effect in 50 % of the subjects

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13
Q

TD50

A

Toxic dose

Concentration which induces toxic effects in 50 % of the subjects

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14
Q

Binding of drug and ligand

A

Ionic/electrostatic interactions form bonds

Usually reversible

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15
Q

Bmax

A

Maximal number of binding sites

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16
Q

KD

A

Concentration of the ligand at which bound and unbound ligand molecules are in equilibrium

Low KD => high receptor/ligand affinity

17
Q

IC50

A

Concentration of a competitor that reduces the binding of a drug to 50 %

Low IC50 => effective competitor

18
Q

Competitive antagonist

A

Binds to the same site on the receptor as the agonist

Antagonist displaces agonist

19
Q

Noncompetitive antagonist

A

Binds to another binding site than the agonist

Increasing the dose of the antagonist does not displace the agonist

20
Q

Major types of drug receptors

A

Ionotropic receptors: gate ion channels directly; e.g. NMDA, AMPA, GABAA

Metabotropic receptors (G-protein coupled receptors, GPCRs): receptor and effector molecule separate; intracellular signalling cascade; e.g. adrenergic, dopaminergic, GABAB, cannabinoid

21
Q

Catecholamines

A

Modulatory neurotransmitterers

E.g. dopamine, noradrenaline, adrenaline

Synthesised from tyrosine by tyrosine-hydroxylase

22
Q

Tyrosine hydroxylase

A

Tyrosine => L-DOPA

Rate limiting enzyme of catecholamine synthesis

Activated by: catecholamines (bind to it), high cAMP, phosphorylation

Inhibited by: high neurotransmitter release, AMPT

23
Q

Alpha-adrenoceptors

A

Bind NA and A equally well, better than agonist isopreterenol

Antagonist: phentolamine

24
Q

Beta-adrenoceptors

A

Bind isopreterenol better than NA and A

Antagonist: Propranolol

Stimulates adenylyl cyclase => more cAMP => stimulates PKA => stimulates CREB

Stimulates heart rate and LTP

25
Q

NA is produced by

A

Locus coeruleus

26
Q

DBH

A

Dopamine-beta-hydroxylase

Dopamine => NA

Needs ascorbate as cofactor

27
Q

VMAT

A

Vesicular monoamine transporter

Transports dopamine from the cytosol into the vesicle

Inhibitor: reserpine, induces vesicle depletion

28
Q

NET

A

Noradrenaline transporters

Transports NA back into the neuron (in striatum: also DA)

NET inhibitors: antidepressants

29
Q

MAO-A

A

Monoamine oxidase A

Metabolises NA, A, serotonine

In outer membrane of mitochondria

Pargyline: inhibitor

30
Q

COMT

A

Catechol-O-methyl-transferase

Metabolises NA and DA

31
Q

Alpha2A-adrenoceptor

A

Presynaptic autoreceptor

Reduces cAMP formation => blocks Ca2+ channels => opens K+ channels => hyperpolarises the neuron => inhibits NA release

Lowering of blood pressure, analgesia, sedation

32
Q

Clonidine

A

Inhibits NA release

Hypotensive, analgetive

Can attenuate symptoms of opiate withdrawal

33
Q
A
34
Q
A

Block C (1 decks)

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