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BIOM2402 Sem 2 > DRUGS 🤯🤕 > Flashcards

DRUGS 🤯🤕 Flashcards

1
Q

Oestrogen

A

Builds endometrium

  • Produced by follicles
  • Negative feedback on GnRH, LH & FSH secretion
  • Tamoxifen competes w estrogen for its R
    Allowing ER dimerisation but preventing co-activators from binding to the dimer on the ERE DNA element
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2
Q

Progestin

A

Stabilises endometrium

  • Produced by follicles
  • Helps implantation of fertilised ovum
  • Negative feedback on GnRH & LH secretion (to prevent ovulation)

Side effects:
- irregular menstrual or vaginal bleeding
- inhibition of luteinising hormone secretion
- reduction in androgen-dependent acne
- prevention of sperm entry into uterus

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3
Q

Inhibin

A

Inhibits FSH secretion to prevent another follicle from forming

Released by corpus luteum (dead follicle that has released egg already)

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4
Q

FSH

A

Stimulates follicle maturation in ovaries

Produced in anterior pituitary

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5
Q

LH

A

Stimulates release of ovum
Produced in anterior pituitary

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6
Q

GnRH

A

Stimulates FSH & LH secretion by anterior pituitary

Produced in hypothalamus

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7
Q

Progestin only pill

A
  • Creates a mucus plug in the cervix to prevent further sperm penetration
  • Prevents LH surge → essentially prevents future ovulation but cannot stop already released egg from being fertilised
  • Oestrogens should not be given without progestins to women with uterus
  • Oestrogens cause hyperproliferation of endometrium = endometrial cancer
  • Side effect of progestin only = irregular menstrual bleeding and high failure rate if improperly used
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8
Q

Combined pill

A

With estrogen:
Estrogen inhibits FSH
Preventing follicle maturation

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9
Q

Hormone replacement for menopause/emergency contraception

A

pretty much same action as two pills but since higher doses they can be used for hormone replacement therapy or for emergency contraceptive

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10
Q

Mifepristone

A

Pregnancy Termination (antiprogestin)

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11
Q

Levonorgestrel

A

‘Morning after’/emergency pill

Progestin competitive inhibitor)
High progestin dose

Prevents LH surge - prevents/delays ovulation

(Only work if taken 2 days before LH surge)
Doesn’t affect foetus

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12
Q

Ulipristal

A

Morning after’ pill

Progestin competitive inhibitor

High progestin dose

Inhibits progesterone binding to receptor (exact mechanism unknown)

Prevents/delays ovulation

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13
Q

Letrozole & Anastrozole

A

P450 Aromatase Inhibitors

Block androgen binding to aromatase active site (more specifically blocks conversion of testosterone to oestradiol and conversion of androstenedione to oestrone).

Reduces oestrogen synthesis

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14
Q

Tamoxifen

A

Oestrogen receptor inhibition

Tamoxifen is metabolised to 4-hydroxytamoxifen by liver (CYP2D6/CYP3A4), entering the cell.

Binds to oestrogen receptor allowing receptor dimerisation but preventing further binding of co-activators, preventing

gene transcription (more specifically oestrogen response elements) in cells

Lack of conformational change of oestrogen receptor results in no gene transcription

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15
Q

Alprostadil

A

(PGE pathway)

Increases PGE1

Injectable into the corpus cavernosa?
Painful (as PGE is an inflammatory molecule).

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16
Q

Papaverine

A

PDE pathway

Unknown - Proposed to inhibit phosphodiesterase 5

Causes vasodilation

Only used if alprostadil is contraindicated
No localised pain

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17
Q

Phentolamine

A

Adrenergic nerve inhibitor

Competitive antagonism of alpha-1 adrenoreceptors

Causes vasodilation

Inhibits the action of adrenergic nerve stimulation which is smooth muscle contraction (think SNS → fight or flight so vasoconstriction in non-essential organs)
By inhibiting this vasoconstriction it promotes vasodilation

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18
Q

Levitra - Vardenafil
Viagra - Sildenafil
Cialis Tadalafil
=Lower dose & longer duration of action

Think ‘fils’ fill the corpus cavernosum with blood through vasodilation

A

PDE5 inhibitors

Take pill 1-2h before intercourse
Still needs stimulation from NANC nerves
prevents degradation of cGMP to 5’-GMP to allow endogenous NO to be more effective

Metabolised/inactivated by P450 3A4

QUICK NOTE HOW SMOKING DISRUPTS DRUG FUNCTION:
Damages Endothelial cell resulting in release of vasoconstrictors, harden blood vessels, decreasing penile blood flow,
Increases RADICALS (superoxide & peroxy nitrite) that decrease NOS activity
Increased SNS (sympathetic nervous system) tone

19
Q

Finasteride
Dutasteride
- Better and more consistent therapy than finasteride
Ideally drug of choice

A

Inhibits 5AR (5-alpha-reductase) and decreases DHT (5-alpha-dihydrotestosterone

Reduces prostate size and reduces pressure of bladder and urethra

Used for benign prostatic hyperplasia (enlarged prostate)

Finasteride can also be used for androgenic alopecia (male pattern balding).

20
Q

Alfuzosin & Tamsulosin

A

Alpha-1A selective (specific for prostate gland and bladder neck)
Less cardiac side effects
Less effective against benign prostatic hyperplasia but also less hypotension

Reduces degree of smooth muscle contraction in prostate to reduce pressure on urethra and increase urinary flow.

Specific for alpha-1 and won’t induce tachycardia via alpha-2 receptors

21
Q

Prazosin & Terazosin

A

Less receptor selectivity
More effective in BPH treatment but dose titration is needed to minimise hypotensive effects
Reduces degree of smooth muscle contraction in prostate to reduce pressure on urethra and increase urinary flow.

Specific for alpha-1 and won’t induce tachycardia via alpha-2 receptors

22
Q

Thalidomide

A

R enantiomer: sedative

S enantiomer: teratogenic

Used for morning sickness due to sedative effects of R enantiomer, but S enantiomer caused birth defects

23
Q

Pilocarpine

A

Muscarinic ACH agonist
SLUDGE BBB

24
Q

Carbachol

A

Muscarinic ACH agonist
SLUDGE BBB

25
Q

Atropine

A

Anticholinergic/competitive reversible muscarinic antagonist
Anti-sludge BBB

26
Q

Muscarine

A

Agonist of muscarinic acetylcholine R
SLUDGE BBB

27
Q

Scopolamine

A

Anticholinergics or Competitive reversible muscarinic antagonist

Anti-sludge BBB

28
Q

Acetylcholine

A

Agonist of nicotinic and muscarinic acetylcholine receptor.
SLUDGE BBB

29
Q

Adrenaline

A

Physiological antagonist of acetylcholine - binds to adrenergic receptors, causing opposite effects.

30
Q

Pyridostigmine

A

Acetylcholinesterase inhibitor ‘stigmines’ - increases acetylcholine concentrations.

SLUDGE-BBB

31
Q

Class I: Antidysrhythmics

Sodium Channel Block (e.g. lignocaine)

A

Block voltage gated sodium channels by preferentially binding to inactivated state, reducing sodium influx and membrane depolarisation.

32
Q

Class II

Beta adrenoceptor antagonism (Beta blockers)

A

Blocks beta 1 and beta 2 receptors
Block sympathetic activity, decreasing cAMP

33
Q

Class III:

Potassium channel block

A

Prolong cardiac action potential, increasing refractory period of sodium channels, preventing reentrant tachycardia and suppressing ectopic activity.

Prolonged plateau phase

34
Q

Class IV:

Calcium channel block (e.g. verapamil and diltiazem)

A

Calcium channel antagonists

Slow conduction in the SA and AV nodes, reduced calcium entry, also reduces the after-depolarisation. Calcium antagonists will also reduce contractile force

Shortened plateau phase

35
Q

Adenosine

A

Acts on adenosine receptors

Makes pacemakers less excitable

Opening of K+ channels and hyperpolarization

Used for tachycardia

36
Q

Atropine

A

Competitive antagonist of muscarinic receptors. Removes the parasympathetic brake on the heart rate

Used for sinus bradycardia

37
Q

Isoprenaline

A

Beta agonist sympathomimetic

produces a positive inotropic and chronotropic effect

Treatment of heart block or bradycardia with haemodynamic compromise

38
Q

Adrenaline

A

Non-specific agonist for adrenergic receptors.

Produces a positive ionotropic and chronotropic effect.

Used for cardiac arrest

39
Q

Ivabradine

A

New drug:
Coronary heart disease
Chronic heart failure

40
Q

Benzodiazepines(BNZ)

A

Antiepileptic drugs

Binds to alpha 1 (VTA) → reduction of GABA release → Increase GABA release

41
Q

Barbiturates

A

Similar to BNZ + inducer of P450s

42
Q

Valproate

A

Is a T-type calcium channel blocker (which is why it is helpful to treat absences, since they are caused by abnormalities in these channels.

43
Q

Calcium channel blockers (e.g. valproate and ethosuximide)

A

Block T-type channels contributing to rhythmic discharges in thalamus involved in absence seizures.

44
Q

Morphine

A

Opioid:

Full agonist of opioid receptor

Via µ opioid receptors (which work as G protein-coupled receptors which inhibit adenylate cyclase activity, open K+ channels and inhibit the opening of Ca2+ channels in nerve endings), opioids inhibit the release of neurotransmitters like substance P from nerve terminals, leading to suppression of asc/desc pain pathway signalling.

Kappa receptors can exert additional effect on spinal cord.

BIOM2402 Sem 2 (14 decks)

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