Basic Science Concepts Flashcards
Chemical structure determines
lipophilicity (lipid loving and can cross membranes easier, less soluble in water, and non polar)
hydrophilicity (water loving, can’t cross membranes s easy, more soluble in water, polar)
structure activity relationship
the structure of the compound and its relation to it’s activity
the functional groups in the compound (part of the chemical structure) determine the mechanisms of action and degredation
Explain the body’s two phase detoxification system’
phase 1 reactions: oxidation, hydrolysis (the body’s main way of excreting drug is renally, so drugs need to become more hydrophilic/polar)
phase 2 (conjugation) reactions: glucuronidation, sulfate conjugation
this is how the body gets non polar drugs/lipophilic/non charged drugs to be polar/hydrophilic/charged so that the metabolite can be sent to the kidney and metabolize
How are drugs degraded
oxidation (loss of electrons) & hydrolysis (water) & then photolysis (light destroys carbon bonds)
these are three mechanisms where sometimes even before a drug reaches a pts mouth, if the drug is not kept properly, it can begin to degrade
Naturally, most drugs are lipid soluble, non charged and non polar but when in the body, it wants to be in more of a hydrophilic state so that the drug can be removed from the kidney and concentrate in the urine – so it is converted through phase 1 and phase 2 reactions to a hydrophilic, polar, charged molecule
morphine is a full agonist at which receptor
a mu opioid receptor
mimics endorphins (which are endogenous)
naloxone is a full antagonist at which receptor
a mu opioid receptor
it competes with the endogenous ligand (endorphins) and even the exogenous ligand (morphine) so that it cannot act anymore
naloxone is a full antagonist at which receptor
a mu opioid receptor
it competes with the endogenous ligand (endorphins) and even the exogenous ligand (morphine) so that it cannot act anymore
competitive inhibition
when the substrate binds directly to the active site of the enzyme and competes with what’s normally supposed to be there
non competitive inhibition
when the substrate binds indirectly, to a different portion of the enzyme and causes the active site to change shape so the normal ligand is not able to fit and cause it’s action
CNS
brain, spinal cord, nerve cells/neurons
PNS break down
peripheral nervous system - somatic (voluntary, muscle) and autonomic (involuntary, heart, BP, GI) bodily functions
Autonomic nervous system communicates with internal organs and glands and there is the sympathetic (arousing) and parasympathetic (calming) division
The somatic nervous system communicates with sensory organs and voluntary muscles for the sensory (afferent nervous system- sensory input) and the motor (efferent nervous system - motor output) - the primary neurotransmitter for somatic NS is Ach, it binds to nicotinic receptors (Nn) in skeletal muscles and affects skeletal movement
CNS and PNS communicate to each other through
neurotransmitters (NTs) that pass through neurons
we dont grow new neurons, but we do grow dendrites in response to positive stress . ex: just like a muscle grows with more stress we have to keep the brain working in the elderly so the neurons/dendrites will keep being healthy
glial cells
they provide nutrition and cohesive support for the neurons life and to keep the neuron healthy
there are two types:
schwan cells and astrocytes
how is signal transmission between the CNS and the PNS accomplished
They communicate via neurotransmitters - the body’s chemical messengers (substrates/ligands). they are released from presynaptic neurons into the synaptic cleft, then they travel to post synaptic neurons or other parts of the body to exert their effect
common neurotransmitters : (Ach), epinephrine (epi)- aka adrenaline, Norepinephrine (NE) aka noradrenaline, dopamine (DA), and serotonin (5HT)
what is the primary NT for the somatic NS and what receptor does it bind to
Ach, it binds to nicotinic receptors (Nn) in skeletal muscles and affects skeletal movement specifically within the somatic nervous system (in autonomic NS they bind to muscarinic receptors)
if people can’t make muscle movements its usually because they lack the neurotransmitter or the receptor that helps to signal motor movements
What are the NT’s involved in the sympathetic nervous system (autonomic) vs the parasympathetic nervous system (autonomic)
sympathetic - fight or flight - uses NE and Epi neurotransmitters on alpha 1 and beta 1 and beta 2 adrenergic receptors in the cardiovascular and respiratory systems, and this leads to decreased urination and digestion and increased HR, BP, increased bronchodilation, and glucose production.
parasympathetic - rest and digest - Ach binds to muscarinic receptor (most drugs) throughout the body like GI system, bladder, eyes; which leads to SLUDD: salivation, lacrimation (tears), urination, diarrhea (defecation), digestion
anti-muscarinic aka anticholinergic = anti-SLUDD aka cant see, cant pee, cant spit, can’t poop
the location of the alpha 1 adrenergic receptor and what are examples of agonists and antagonists
smooth muscles
blood vessels
Agonist: vasoconstrictors - dopamine (an inotrope that raises BP to increase CO), oxymetazoline (afrin nasal spray)
Antagonist: phentolamine (nonselective for alpha 1 and alpha 2 adrenergic receptors)
the location of beta 1 receptors and example agonist and antagonists
heart
agonist - dobutamine (inotrope that increases HR and increases CO)
antagonist - metoprolol (decreases HR and decreases BP, antihypertensive that also used in HF)
the location of beta 2 receptors and example agonist and antagonist
lungs
agonist - albuterol (short acting, used for asthma and COPD, causes bronchodilation
antagonist - propranolol (This is a beta 1 and beta 2 blocker - AVOID IN COPD because it can cause bronchoconstriction and hinder breathing)
endorphins are
endogenous hormones secreted in the brain and nervous system that active the body’s opiate receptors and cause analgesia
the exogenous versions are these are opioids that bind to mu- receptors like morphine
pyridostigmine is a drug used for myasthenia gravis because
it is an acetylcholinesterase inhibitor so it allows Ach to be around longer in order to have an affect on the muscle/motor function
This is also known as a cholinergic drug or a nicotinic agonist
Neostigmine is a drug that is used to reverse paralytic drugs, how?
It reverses the non-depolarizing neuromuscular blockers that work to intentionally antagonize Ach and prevent muscle function. this drug pretty much reverses all of the neuromuscular blockers besides succinylcholine because it is a depolarizing neuromuscular blocker
This is known as a cholinergic drug or a nicotinic agonist
Succinylcholine MOA
MOA: the only depolarizing neuromuscular blocker (all others are non depolarizing) and it binds to nicotinic Ach receptors and prevents the ACh from working leading to temporary paralysis
Example of alpha 2 agonist and antagonist
An alpha 2 receptor agonist inhibits sympathetic activity and lowers blood pressure
agonist - clonidine (antihypertensive that relaxes arteries and increases blood supply to heart which then lowers BP and HR)
antagonist - yohimbine aka yohimbe (helps with erection by vasodilation
Which receptor does dopamine go to
alpha 1 or beta one depending on the dose!
MOA of benzodiazepines
They bind to and enhance the effect of inhibitory neurotransmitter GABA - which causes anxiolytic, hypnotic, anticonvulsant, and muscle relaxant effects (including relaxing the diaphram which could lead to respiratory suppression)
they shouldn’t be taken with opioids because opioids can do the same thing. they both have boxed warnings for use together causing profound sedation, respiratory , coma, death.
Box warning for benzos and opioids
benzos shouldn’t be taken with opioids because opioids can do the same thing. they both have boxed warnings for use together causing profound sedation, respiratory depression, coma, death.
restrict dosages and duration, monitor patients for signs and symptoms of respiratory depression/sedation
True or false: since the MOA of Tylenol and opioids is different, the drugs work synergistically and there’s not increased risk of respiratory depression
True. They can be taken together safely
pharmacokinetics is ADME
PK drug interactions occur when one drug alters the absorption, distribution, metabolism, or excretion of another drug and they can be beneficial or harmful interactions
