Pharm II Flashcards by Eric Sun

M2/M4/alpha2 receptor couples to __ and cause ___?

Gi/decrease in cAMP or hyperpolarization

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M1/M3/M5/alpha1 receptor couples to ___ and cause ___?

Gq/increase DAG and IP3

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Beta1/2/3 receptor couples to ___ and cause ___?

Gs/increase in AC and increase in cAMP

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What is autoreceptor?

Presynaptic receptor that response to the NT released/usually inhibitory

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What is heteroreceptor?

Presynaptic receptor that response to the NT other than the one released

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What is the normal state of Fe in hemoglobin?

Ferrous 2+

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What is the route of CO’s absorption and excretion?

Respiration

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How do we know if it methylene chloride that is causing the CO poisoning?

CO levels rises after removal from the source

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What is carboxyhemoglobin?

CO + hemoglobin

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Carboxyhemoglobin shifts the O2 dissociation curve to the ___?

Left

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Does the level of carboxyhemoglobin cause all the toxic effect of CO poisoning?

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Which enzyme in mitochondria does CO binds to?

Cytochrome oxidase—>inhibit cellular respiration

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How is peroxynitrites form?

CO displaces nitric oxide from platelets—>free radical damage

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What are some severe CO acute clinical findings?

Coma/seizures/HoTN/MI

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What does the CO late effect cause?

Neurologic effects from lipid peroxidation

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The __ you are the higher risk for delayed neurologic effect of CO

Older

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What is O2 saturation for CO poisoning?

Falsely normal for pulse oximetry

Co-oximeter for arterial blood gas is appropriate (if use old blood gas machine then it is falsely normal)

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How to treat CO poisoning?

Give O2 to shorten CO half life/hyperbaric (2.8 atm)—>shorten CO half life and prevent lipid peroxidation

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When do we give HBO?

LOC/GCS

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What do we see on the brain MRI for delayed neurological effect of CO?

Bilaterally low density areas of the globus pallidus

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Why is there an increase of lactate (>10mmol/L) in cyanide poisoning?

CN binds to cytochrome A3—>no ATP—>lactate level goes up

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Why do we use nitrite (e.g. sodium nitrite) for CN poisoning?

Nitrite convert hemoglobin to methemoglobin (Fe 3+)—>CN prefer Fe3+ therefore ditch cyt A3 to bind with methemo—>forms cyanometHb—>don’t bind O2, better than no ATP

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What role does thiosulfate play in CN poisoning?

enhance normal metabolism of CN

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Why can’t we use nitrite for CN AND CO poisoning?

MetHb further lowers O2 carrying capacity

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What does H2S gas do?

Similar to CN but its binding is reversible

What is hyroxycobalamin?

Bind to CN and form cyanocobalamin (vitamin B12)--->also increase BP a bit--->usually used with thiosulfate

How many antidote do we use for CN crystal poisoning?

Nitrite/thiosulfate/hydroxycobalamin

Sign of MetHb poisoning?

O2 doesn't help/pulse oximetry is falsely lower/co-oximeter is appropriate

What is the antidote for methemoglobinemia?

Methylene blue

What is the mechanism of methylene blue?

Cofactor for NADPH reductase (reduce MetHb to normal)--->gain e- from NADPH--->give it to MetHb

Why pt with G6PD deficiency does not respond to methylene blue?

G6PD is needed to convert methylene blue back to the reduced form (working form)

What is sulfHb?

Sulfer + Hb--->can't carry O2--->similar to MetHb

How to distinguish sulfHb/MetHb?

Give pt CN--->if CN levels drops then it is MetHb

Bronchoconstriction is driven by M_ receptor?

What are the 2 kinds of cholinoceptor stimulants?

Direct and indirect (inhibit acetylcholinesterase)

What are the features of Bethanechol?

Muscarinic selective/stable/relieve urinary paralysis after surgery/poorly absorbed by CNS because of quaternary ammonium group

Which muscarinic receptor mediate the production of EDRF (endothelial derived relaxing factor)?

M3 on endothelial cell--->NO--->cGMP--->decrease Ca2+--->vasodilate

How does the indirect acting carbamate drugs inhibit cholinesterase?

By covalent bond to the enzyme and temporarily occupy it (takes a while for it to be hydrolyzed)

How does the indirect acting non-ester drugs inhibit cholinesterase?

Bind to the enzyme as long as it is not metabolized

How does the indirect acting organophosphate drugs inhibit cholinesterase?

Irreversibly inactivate the enzyme

What does pralidoxime do?

Reverse the damage done by the organophosphate drugs--->regenerate cholinesterase (can't regenerate the enzymes that have gone through aging process--->can't bring the enzyme level back to 100%)

What happens if you give too much cholinesterase inhibitors to a pt?

Muscle strength would go up and then paralysis (for both healthy and Myasthenia gravis pt)--->edrophonium (short lived) is used to determine under or overdosing

What is SLUDGE (too much ACh activation)?

Salivation/lacrimation/urination/defecation/GI distress/emesis

What is atropine?

ACh analog--->competitively inhibit muscarinic receptor

Why used tropicamide instead of atropine to dilate your pupils?

Tropicamide has a shorter half life

What do we use for overdose of direct acting muscarinic agonist?

Atropine

What do we use for overdose of indirect acting muscarinic agonist?

Atropine and pralidoxime

Which receptors are most sensitive to atropine?

autoreceptor in the heart (react to low dose of atropine)

How to treat children with atropine overdose (atropine fever)?

Treat symptoms rather than using AChE inhibitor

What is the similarity between Succinylcholine and Mivacurium?

Both short lived

Cholinesteras inhibitor can reverse the effect of non or depolarizing NMJ blocker?

Nondepolarizing blocker (since it was competitively inhibited)

Malaria enters the body and goes to __ first?

Liver

Primaquine induce anemia in pt with ___ deficiency?

G6PD

P. malariae/knowlesi does not have any resist to ___

Chloroquine

Use ___ for falciparum/malariae/knowlesi

Chloroquine

Use ___ for vivax/ovale

Chloroquine + primaquine (prevent relapse)

For chloroquine resist falciparum, use ____

Atovaquone + proguanil (chloroguanide)

For chloroquine resist vivax, use ____

Quinine + doxy or tetra + primaquine

What is the rate limiting layer of the skin for percutaneous absorption?

Corneum through con. gradient

Topical drug is absorbed via ___?

Passive diffusion

2 factors that can enhance percutaneous absorption?

Hydration/skin disease (eczema)/some disease might hinder like ichthyosis vulgaris

What are the 3 categories of vehicles and their examples?

Monophasic: powder/oil/liquid Biphasic: lotion (powder + liquid)/paste (ointment + powder/cream (oil + liquid)

Features of powder?

absorb moisture and reduce friction/can increase friction if clumped

Features of gels?

Liquid that is converted into semisolid/used in hairy areas

2 way to prepare cream?

Oil in water (evaporate/drying)/water in oil

Features of ointment?

Little to no water

Risk of class I topical steroid?

Can cause steroid atrophy (decreased collagen)/cause glaucoma if applied near the eye

What is occlusion for dermatology?

Wear something over the topical medication to drive it into the skin

Systemic affect of topical steroid is?

Suppression of hypothalamic-pituitary-adrenal axis

What kind of UV light is used for psoriasis treatment?

UVA and UVB (UVC is absorbed by the ozone layer)

Long term treatment of UVA leads to ___?

Skin cancer

What does the UV light do treating psoriasis?

Immune suppress (for inflammatory conditions)

Why is psoralens (naturally in lime) used with UV light?

Enhance absorption

Can medication be photosensitizing?

Yes

What does sunscreen do and what is SPF

Scatter and absorb UV rays/for example: it takes 2 hours for you to get red in the sun, SPF 15 will take 2x15=30 hours for you to get red

How often should you reapply sunscreen?

around 2 hours

Does sunscreen prevent you from getting Vitamin D?

Yes

Why use MTX for psoriasis?

Psoriasis: increase skin cell turn over MTX: inhibit cell growth

What percentage of MTX is bound to plasma protein?

50%

Psoriasis is a ___ disease

Systemic

Side effects for biologic treatment (DMARD/TNF alpa inhibitor and what not)?

Risk of infection/site reaction/unmasking neurologic diseases

Don't use MTX for psoriasis if the pt has?

Liver/GI/want babies/pulmonary diseases

Don't use UV for psoriasis if the pt has?

History of skin cancers

What does retinoid do for psoriasis?

Normalize epidermal differentiation

Retinoid causes?

Fetal abnormality (don't give to pregos)

Phase of inflammatory responses?

Acute (increase capillary permeability)--->subacute (leukocytes infiltration)--->chronic (necrosis)

What does histamine do?

Capillary dilation/increase post-capillary venule permeability/sensitizing sensory neurons (itching)

Difference and similarity between kinins and histamine?

Similar effect/kinin is more long term/kinin also increase arachidonic acid release

Difference and similarity between COX1 and COX2?

Both metabolize arachidonic acid/COX1 is always been made/COX2 is made during inflammation

Goals for NSAIDs?

Relieve pain/slow tissue damage/inhibit COX1/2

How does aspirin work?

Put an acetyl group onto COX1/2 and irreversible block the making of eicosanoids

Salicylic acid (hydrolyzed form of acetylsalicylic acid) can ___

Reversibly inhibit COX1/2

Effect of aspirin?

anti-inflammatory/analgesic/antipyretic/inhibit TXA2--->increase bleeding time

Dosage progression of aspirin

Anti-platelet (low dose)--->analgesic and antipyretic--->anti-inflammatory

Acetaminophen overdose is resulted from the depletion of ___?

Glutathione

Indomethacin should not be used for___?

Children

Selective COX2 inhibitor is not ___ like traditional NSAIDS

anti-platelet

Where is norepi converted to epi?

In adrenal medulla

Difference between norepi and epi (besides epi can bound to beta 2)

Norepi is a NT/epi is a neurohormone

Alpha methyl tyrosine ___ the synthesis of NE

Decreases

Beta 1 increase ___ and ___?

HR and force of contraction

Beta 3 increases ___?

Lipolysis

Beta is more ___ than alpha, therefore low dose affect ___ first? and high dose affect ___ more? (skeletal muscle)

Beta is more sensitive/low dose (body) affect beta first/high dose (drug) affect alpha more

Which is more potent for all receptors, NE or epi?

Epi

Iso/NE/epi, who is the most potent for beta receptors?

Iso

Why does NE release decrease if you keep giving tyramine?

NE pool is gradually depleted

What chemical structure predict indirect acting drugs?

OH group on benzene ring and acyl side chain