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Pharmacology RCOA > Pharmacology basics > Flashcards

Pharmacology basics Flashcards

1
Q

What are aliphatic compounds?

A

Contain carbon chain with functional groups attached

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2
Q

What do all aromatic compounds contain?

A

Benzene ring

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3
Q

How does barbituric acid become active?

A

Addition of phenyl group = anticonvulsant
Addition of alkyl group = hypnotic

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4
Q

What happens if O2 is substituted for Sulfur in Barbituric acid?

A

Increases solubility allowing drug to cross BBB

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5
Q

How are volatiles divided?

A
  • Ethers (Iso/Sevo/Desflurane)
  • Halogenated hydrocarbons (Halothane, Chloroform)
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6
Q

How is a halogenated hydrocarbons potency & stability increased?

A

Potency: Chloride/bromide
Stability: Fluoride

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7
Q

What are the compounds found in local anaesthetics?

A

Aromatic group
Amine group
Intermediate chain

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8
Q

What are the 2 main functional groups in LA?

A

Ester
Amide

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9
Q

Which anaesthetics are esters?

A

Procaine
Tetracaine

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10
Q

Which LA are amides?

A

Lidocaine
Bupivacaine

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11
Q

What does the type of linkage in an LA determine?

A

Speed of metabolism
Esters = Fast, by plasma esterase
Amides = Slowly, in liver

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12
Q

What increases the potency/duration of a LA?

A
  • Increased lipid solubility
  • Protein binding (inc amide side chain or add groups)
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13
Q

What makes a molecule an acid or a base?

A
  • Acid = Molecule that donates protons
  • Base = Molecule that accepts protons
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14
Q

What is the role of the functional group of a drug?

A

Affects whether drug is an acid or base

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15
Q

What happens to Midazolam at physiological pH?

A
  • Contains amine group
  • Amine group incorporated into benzodiazepine ring
  • Renders drug non-ionised, lipid soluble
  • Able to cross BBB
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16
Q

What happens to Thiopental in a pH of 10 and pH 7.4?

A
  • 10: Ionised and water soluble
  • 7: Non-ionised lipid soluble molecule able to cross BBB
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17
Q

What are the properties of ionic compounds?

A
  • Electron transfer
  • High melting & boiling points
  • Soluble in water
  • Conduct electricity
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18
Q

What elements tend to form covalent bonds?

A

Non-metallic e.g oxygen

19
Q

What affects the polarity of a molecule?

A

The electro-negativity

20
Q

Why is Desflurane metabolised slower than Isoflurane?

A
  • Desflurane has higher electro-negativity
  • Results in stronger bonds
21
Q

What are the 3 types of attraction between molecules?

A
  • Van der Waals forces: Weakest
  • Dipole-Dipole: Attraction between polar molecules
  • Hydrogen bonding: Strongest, H+ bonded to strongly electronegative atom
22
Q

How does intermolecular attraction affect GA?

A
  • GA acts by disrupting molecular associations due to VdW/Hydrogen bonds within lipid membranes
  • Includes the H+ bonds in OH & NH groups formed within neurotransmitters receptors
  • Also formation of H+ bonds e.g aromatic rings & volatiles
23
Q

What are most types of bonds between drug and receptor?

A

Ionic

24
Q

How do bonds work on acetylcholine?

A
  • +vely charged ammonium ion forms ionic bond with -ve receptor
  • VdW force between CH3 group on ach & receptor reinforces stability
  • H+ bond
25
Q

How is a covalent bond broken?

A

1) Homolytic fission: Each element takes 1 electron to form a free radical (Needs UV or high temp)
2) Heterolytic fission: 1 element takes both electrons so 2 oppositely charged ions formed

26
Q

What makes molecules water soluble?

A
  • Ability of compound to disrupt normal attraction between H2O molecules (due to Hydrogen bonding)
  • Functional groups in a drug can provide regions that can polarise their electron cloud allowing interaction
27
Q

What is pKa?

A
  • The pH at which the conc of the proton donor form is equal to that of the proton acceptor form
  • Indication of how readily a functional group gives up/accepts a proton to become ionized
28
Q

What do the nitrogen atoms on neuromuscular blocking agents do?

A
  • Reduces lipid solubility
  • Increases water solubility
29
Q

What are the cell surface receptors and what is their function

A
  • G protein coupled: Hormones, neuropeptides, neurotransmitters
  • Ligand gated: synaptic transmission (Cys-Loop receptors, Glutamate recepts, P2X recepts, CNG channels, TRP)
30
Q

What are the intracellular receptors and what is their function

A
  • Steroid receptors: Steroids, Thyroxine, Vit D, Retinoic acid
31
Q

What are the enzyme-linked receptors and what is their function

A
  • Tyrosine Kinase: Peptide GF, GH, Cytokines, Prolactin
  • Tyrosine Phosphatase: Unknown
  • Serine Kinase: Transforming GF B
  • Guanylate Cyclase: ANP
32
Q

How do G-Protein Coupled receptors work?

A
  • 7 transmembrane domains coupled to intracellular heterotrimeric G Protein complex
  • Activated by ligand binding
  • Induces conformational change leading to dissociation of G protein
  • Reduces receptor-ligand affinity results in agonist release
  • Alters conc of 2nd messenger molecule or produces a change in membrane potential
  • Modulate funciton of downstream proteins to produce cellular response
  • Intrinsic GTPase activity allows returning to resting state
33
Q

How do ion channels work?

A
  • From aqueous channel in lipid bilayer allowing charged particles to pass
  • 2 types: Voltage-gated & ligand-gated
34
Q

How do voltage-gated ion channels work?

A
  • Open/close in response to changes in voltage across membrane
  • Alpha subunit forms channel pore
  • Confers both ion selectivity & sensitivity
  • Other subunits stabilise & modulate function
  • At normal MP channels are closed
  • When membrane depolarised channels have conformational change allowing them to open
35
Q

How do ligand-gated ion channels work?

A
  • Open in presence of extracellular ligands
  • Inotropic: Binding site & transmembrane ion channel integral to 1 protein. Binding alters activity- rapid synaptic transmission
  • Metabotropic: Transmitter binding site & effector are separate. Coupled via G-protein which alters activity- slower onset
36
Q

What does the Cys-Loop receptor family include?

A
  • Nicotinic Ach receptors (Excitatory)
  • Inotropic serotonin (5-HT3) (Excitatory)
  • GABA A (Inhibitory)
  • Glycine (Inhibitory)
    Each receptor has 5 homologous subunits - 4 transmembrane segments & extracellular N-terminus for neurotransmitter binding
37
Q

How do Tyrosine Kinase receptors work?

A
  • Molecule binds
  • Kinase activity stimulated
  • Tyrosines are phosphorylated
  • Intracellular proteins bind to phospho-tyrosine docking sites
38
Q

What receptors are linked to cytoplasmic enzymes?

A
  • TNF
  • Cytokines
  • Integrins
  • IL-1 receptors
    Important in post-op inflammation, immune response, allergies, pain & tissue repair
39
Q

What is constitutive activity?

A
  • GPCRs able to spontaneously become active without agonist/ligand attachment
40
Q

What are drug receptor binding sites described as?

A
  • Orthosteric: Endogenous activators bind
  • Allosteric: Modulatory sites distinct from the active site
41
Q

What are allosteric functions?

A
  • Drugs binding at multiple distinct binding sites distant from agonist binding sites
  • Causes changes altering receptor function
42
Q

What is signal amplification?

A
  • Usually receptors coupled to enzymes
  • Binding initiates cascade of intracellular responses eg activation of second messenger molecules
43
Q

What is signal dampening?

A
  • Limits physiological response to drug
  • Receptors undergo desensitisation via downregulated expression, receptor internalisation by endocytosis or receptor phosphorylation
  • ## Seen as tachyphylaxis or tolerance

Pharmacology RCOA (10 decks)

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