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ANS/ENS

ATROPINE Muscarinic antagonist. Used for mydriasis, and to


inhibit parasympathetic bradycardia (from stretching) in surgery. An
antagonist would be cholinesterase inhibitors, because they
increase muscarinic activity.nor
ACh Most common in ENS
*Serotonin, Dopamine, NA 5-HT4 on cholinergic motor neuron,
5-HT3 on sensory for anti-emetic, analgesic. axo-axonic synapse,
Dopamine D2 inhibitory
Opioid peptides Opioids stimulate segmental contraction, not
longitudinal. Continuous constipation in heroin addicts (segmental
only). Useful against travellers diarrhea.
Ipecacuanha syrup induce vomiting
Apomorphine dopamine agonist to induce vomiting
ANTIEPILEPTIC
Phenobarbital/Diazepam GABAergic drugs.
Barbituates/benzodiazepines. They increase inhibition of GABA,
dont work by themselves. Drowsiness/cognitive problems
associated, hence used as sedatives (gets better with time).
Diazepam is opening probability, phenobarbital is opening time.
Carbamazepine, phenytoin, valproic acid sodium channel
blockers for epilepsy
Ethosuximide Block calcium channels at synapse. Useful for
absence seizures.
AMPA/KA-R blockade (topiramate) blocks glutamatergic
NMDA-R (felbamate) blocks glutamatergic (last resort)
ENDOCRINE
Vasopressin kidneys, retain water (V2) and constrict peripheral
blood vessels (V1). Diabetes insipidus, local vasoconstrictor
ACTH adrenocorticotrophic hormone (stimulates adrenal cortex)
CRH
TSH stimulates thyroid TRH
GH growth hormone GHRH (somatotropin) and GHIH
(somatostatin) causes IGF-1 release, increases protein synthesis,
as well as other growth including bone growth.
Cortisol glucose-sparing hormone. Tendency to hyperglycemia.
Cushings syndrome.
T3 and T4 thyroid hormones
Carbimazole, Methimazole, Propylthiouracil thyroid
peroxidase inhibitors, blocks T3 and T4 (not for nursing mothers!)
GnHRH makes LH and FSH. These come from anterior, has
tropic and non-tropic, act on ovary to produce oestrogen and
progesterone in ovary. HPO axis. Pulsatile GnRH. FSH on GF cells
(oestrogen), LH on ovary corpus luteum, progesterone. Positive or
negative loops.
ANTIARRHYTHMIC

Lidocaine, flecainide Class I antiarrythmic drug. Keeps sodium


channel in inactivated for longer. Bind to alpha subunit, reducing
rate of depolarization, preventing propagation. Important for
tachyarrhythmia. Lidocaine blocks in between 1 heartbeat. Used a
lot for ventricular dysrhythmias.
Propranolol/Atenolol atenolol is B1 specific, both are beta
antagonists. Decrease refractory period at AV node to prevent
supraventricular tachycardias. Bronchospasm, reduction in
contractile force and bradycardia.
Amiodarone, sotalol Prolong the action potential acting on K+
channels. Sotalol is also partially beta-antagonism.
Verapamil, diltiazem long-lasting calcium channels. Block L-type
channels. Slower conduction in SA and AV. Helps with afterdepolarization. Less contraction.
Digoxin cardiac glycoside that increases cardiac force, blocks
Na/KATPase. Stops after-depolarization, but that causes increased
twitch tension. Narrow therapeutic index
ANTIPLATELETS
ADP/Thromboxane activates platelets
Prostacyclin/NO Stops activation of platelets
Aspirin Stops cyclo-oxygenase, stops platelet aggregation (not
aggregation stopping because endothelial are resistant).
Clopidogrel major P2Y12 antagonist, stopping effect of ADP to
activate platelets. Well-absorbed prodrug. Varying response due to
Cyp2c19.
Abiciximab/Tirofiban GPIIb/IIIa inhibitors. Abiciximab can only be
used once (immune response). Tirofiban avoids some of this, but not
orally absorbed.
ANTICOAGULANTS
Thrombin Activates PAR1/PAR4 and necessary to convert
fibrinogen to fibrin
Heparin Mucopolysaccharides, s.c. or i.v., degraded in stomach.
Increases affinity of anti-thrombin 3 for IIa and Xa proteases. Also,
direct with IIa (thrombin).
Enoxaparin (LMWHs) Cant effect IIa but effects Xa similar to
other heparins. <10kDa
Protamine Sulphate inactivates heparin, treatment for
haemorrhage.
Hirudins Direct thrombin inhibitors. Stop thrombin, stop fibrin.
Comes from leaches. No antidote
Warfarin Vitamin K antagonist, stops vitamin K reductase for
factors II, VII, IX, X. Orally. Bad index, pharmacogenomic problems
(binding and metabolism).
Streptokinase fibrinolytic drug. Activates plasmin to break down
fibrin, useful in venous thrombosis. Short window of time to use for
MI. Immunogenic. Recombinant is slightly better selectivity.

UTERINE
Oxytocin injected slowly, contract smooth muscle of breast and
uterus. OTR GPCRs (Gq, more Ca). Stopped postpartum
haemorrhage, milk
Prostaglandins (PGE2, PGF2, PGI2) converts membrane
phospholipid to arachidonic acid, then PGH2 (COX1 and COX2).
GPCRs. PGI2 (IP) vasodilation for blood to uterus, PGF2 (FP) uterine
contraction, PGE2 (EP) uterine contraction.
Misoprostol/Dinoprostone prostaglandin analogue (Dino is real).
EP, to contract. Induce labor, early terminations, post-partum
haemorrhages. Applied intravaginally. Cervical ripening as well.
Carboprost PGF2 analogue. Also early termination, contraction
etc.
Ergometrine ergot alkaloid. Needs to be relaxed. Used for
postpartum haemorrhage. 1. 5-HT3 ligand-gated receptors and 2.
Alpha-adrenoceptors for vasoconstriction.
Atosiban OT receptor antagonist, stops oxytocin stimulating
contracting. Halts preterm labor (before 37th)
Nifedipine/Magnesium sulfate L calcium channel block,
immediately stops premature labor.
Turbutaline Beta-2 receptor on smooth muscle. Produces cAMP to
relax cell (reuptake of Ca), down PKA for myosin
Ethinylestradiol similar to oestrogen but longer half-life (lasts a
day). Acts like oestrogen. Orally active unlike normal oestrogen.
Inhibits FSH via negative feedback. No GF follicle. Doesnt work
directly.
Norethistrone/Levonorgestrel progesterone analogue. Much
longer half-life. Stops LH via negative feedback on anterior pituitary.
Prevents spike. Used in conjunction with EE.
Mifepristone antiprogestin. Antagonist at progesterone receptor.
Twice the affinity. Medical alternative to surgical termination.
Breakdown of decidua
Gemoprost prostaglandin for expulsion.
Tamoxifen binds to ER as antagonist (doesnt cause gene
activation), stops cancer proliferation. Obviously, side-effects:
partial agonist on ER receptors in endometrium. Endometriosis. Can
become resistant
Anastrozole/letrozole competitive inhibitors of aromatase
enzyme. May mean more testosterone and androstenedione in
women. Good for metastases.
Premarin pregnant mares urine. Lots of oestrogens. Oestrone
sulfates (hydrophilic)
Tetrodotoxin Physically block sodium channels in neuronal cells.
Reversible eventually.
Botox/Spider toxin Stops neurotransmitter release via snare
proteins. Reinjections required for spasms. Spider toxin promotes
release.

Sarin Nerve gas. Stops breakdown in synapse. Dumbels. Need


atropine
Ketamine anaesthesia and analgesia. Glutamatergic NMDA antag.
Also binds opioid receptors.
Memantine Alzheimers. PCP also used (blocks the pore of
NMDA). Glutamatergic. Also noncompetitive. Helpful because it
subtlety blocks pore, stopping excitatoxicity from neuronal death.
Baclofen treat spasticity, works on GABAb, inhibition of release
presynaptically and some postsynaptically.
Strychnine Glycine antagonist, a gruesome poison. Convulsant.
Tetanus Blocks glycine release (not receptors), lockjaw.
Bromocriptine agonist on receptors to suppress prolactin
secretion if youre taking D2 agonist. May be emetic.
L-Dopa Helps with parkinsons (more dopamine). Used in
conjunction with dopa-decarboxylase inhibitor for the periphery.
Only short-term, can lead to unwanted movement.
Entacapone COMT inhibitor, peripherally blocks, counteracts LDopa fluctuations
Domperidone helps with vomiting, dopamine antagonist
(hopefully only in vomiting center)
Cocaine Blocks DAT, increases dopamine in mesolimbic and
mesocortical. Long-term, decreases D2 receptors (hence
parkinsons)
Amphetamine Euphoria is DA effects, also NA effects (jittery).
Interferes with VMAT. Also effect autoreceptors to release dopamine.
High-dose also enzymatic, MAO inhibition and NA effects.
Insulin short peptide, glucose homeostasis.
Sulphonylureas Bind to ATP sensitive K channel, so more insulin
is released.
Biguanides (metformin) activates AMPK, I have lots of energy,
inhibits gluconeogenesis and increases glucose uptake. Weight loss.
Alpha-glucosidase inhibitors (Acarbose) stops/slows
breakdown of sugars (amylase). Never absorbed.
Thiazolidinediones work on liver/adipose tissue. Increase
glucose uptake, decrease gluconeogenesis. Nuclear receptors PPARy.
Improved insulin sensitivity.
ADDICTION
Opiates (morphine, codein, methadone) Hydroxyl groups
make BBB crossing difficult. Heroin and codeine are better. Morphine
is used for severe pain, MI and cancer. Codeine in cough mixtures.
Naloxone/naltrexone opiate competitive antagonist.
Fentanyl/Meperidine Fen synthetic strong opioid agonist. A
patch (potent) for severe or chronic pain.
Methadone Gets people off heroin addiction. Does not give
euphoria (not so BBB), no withdrawal. Lethal in overdose.

Buprenorphine Mu-opioid partial agonist, suppressing withdrawal


and cravings. No incentive to overdose. Sublingual in with naloxone
in system (an antagonist!!!)
Caffeine bronchodilator, mild diuretic. Blocks A2a adenosine
receptor, blocks ability to relax/sleep. At high concn, inhibits
phosphodiesterase, increasing cAMP. Improve concn, motor skills,
no euphoria.
ADDICTION 2
Novocaine (procaine) not as addictive as cocaine. Takes a long
time to have effect. Wears off very quickly, not as potent.
Vasodilation, so absorbed away. Adrenaline is added to combat this.
Allergic reactions. Combination with penicillin for slow absorb.
Lidocaine (lignocaine) not allergic. Very quickly, anaesthesia for
several hours. Also an antiarrhythmic drug. Stingoes. Also needs
adrenaline (not in cutaneous).
Bupropion inhibit neuronal reuptake. Also, non-competitive
antagonist at nicotine. Better than nicotine replacement surgery.
May cause seizures.
Disulfiram slows aldehyde dehydrogenase, causing acetaldehyde
which makes lots of bad side effects aversion therapy for
alcoholics
Ethanol GABA-mediated inhibition, with BNZ causes CNS
depression. And, inhibition of function of NMDA glutamate. Inhibits
calcium channels. Disinhibition of reward pathways. Inhibits release
of ADH.
Cannabinoids (THC) Psychomimetic/depressant. Decreased
intraocular pressure (glaucoma). CB1/CB2 GPCRs, potassium out,
hyperpolarize. Hence, sedative. Not brain stem not respiratory.
Nausea and vomiting after chemotherapy, analgesia, stimulation of
appetite (AIDs)
RESPIRATORY
Salbutamol Beta agonist. SABA
Salmeterol LABA. Not recommended, stops normal ANS function,
masks increasing problem
Montelukast and zafirlukast CysLTs inhibitors. Affect
eosinophils, mucous glands, CysLT receptor 1. Orally
Theophylline, aminophylline xanthines. Lots of side effects.
Inhibit PDE incr cAMP/cGMP relaxation.
Cromoglycate/Nedocromil phrophylactic. Inhalation
Budesonide/Fluticasone/Ciclesonide can stunt growth, but
effective maintenance.
Omalizumab anti IgE. C3 domain. FEV1??