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My pharma notes > Notes from the first 3 practical powerpoints > Flashcards

Notes from the first 3 practical powerpoints Flashcards

1
Q

Usual size of drugs, molecular weight

A

most are 100-1000 g/mol

drugs with MW more than 1000 are limited by diffusion

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2
Q

CYP450 inhibitors

A

SICKFACES.COM, G

Sodium Valproate
Isoniazid
Cimetidine
Ketoconazole
Fluconazole
Acute Alcohol
Chloramphenicol
Erythromycin - Macrolides
Sulfonamides
Ciprofloxacin
Omeprazole
Metroniddazole
Grapefruit Juice.
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3
Q

CYP450 Inducers

A

CRAP GPS

Carbamazepines (phenytoin)
Rifampicin
Alcoholism
Phenytoin
Griseofulvin
Phenobarbitone
Sulphonylureas
Chronic alcohol
St John's wort
Phenytoin
Phenobarbital
Nevirapine
Rifampin
Griseofulvin
Carbamazepine.

Chronic alcoholics Steal Phen-Phen and Never Revamp Grandpas Carbarator.

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4
Q

What is the NOAEL

A

No observed adverse event level.

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5
Q

What is the modified therapeutic index?

A

TD10/ED90

Toxic dose 10% / Effective dose 90%

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6
Q

What is the safety index?

A

TD1/ED99

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7
Q

Therapeutic index?

A

humans TD50/ED50

animals LD50/ED50

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8
Q

What are the drugs with a narrow therapeutic index?

A 
Warning My Phriend, These Drugs are Lethal
Digoxin
Lithium
Theophylin
Warfarin
Phenytoin
Methotrexate

Warning, These Drugs are Lethal

Warfarin, Theophylin, Digoxin, Lithium

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9
Q

Nicotinic receptor structure and subtypes

A

Nm - muscle NMJ receptors, can be embryonic, alpha1, beta1, gamma, and delta subunits. 2:1:1:1, or adult: alpha1, beta1, delta, and epsilon. 2:1:1:1

Nn - neuronal receptors. Many kinds, can be homomeric or heteromeric. 10 different alpha subunits, 4 different beta subunits and many others.

Minimum of 2 ACh ligands are required for opening. 2-5 depending on type.

ACh binds receptors at junctions between alpha-alpha junctions or alpha-beta, alpha-epsilon/delta junctions

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10
Q

Where do spasmolytics act?

A

In the CNS, decrease muscle tone

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11
Q

Where do muscle relaxants act?

A

Pre or post synaptically at the peripheral NMJ.

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12
Q

Presynaptic muscle relaxants (list)

A

Botulinum toxin
Omega-conotoxin

Aminoglycoside and tetracycline side effect

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13
Q

Post synaptic muscle relaxants (list)

A

Curare derivatives - Isoquinolines and Steroids

Depolarizing agents - Succinylcholine

Ryanodine antagonists

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14
Q

Isoquinoline muscle relaxants

A

Tubocurarine

Mivacurium
Atracurium
Cisastracurium

Doxacurium

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15
Q

Steroid muscle relaxants

A

Pancuronium
Pipecuronium
Vecuronium
Rocuronium

Pan Pipe Vec Roc

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16
Q

Which muscle relaxants are metabolized by the liver, and need to have dose reduced in liver disease?

A

Vec Roc
Vecuronium
Rocuronium

17
Q

Which muscle relaxants are excreted unchanged in the urine?

A

Pancuronium and Pipecuronium

18
Q

Which muscle relaxant can release histamine?

What is its other dangerous side effect?

A

Atracurium releases histamine

Laudanosine, the atracurium metabolite, can provoke seizures.

19
Q

What is the short acting muscle relaxant?

How is it metabolized?

A

10-15 minutes
Mivacurium

By pseudocholinesterase/Butrylcholinesterase.

20
Q

What are the long acting muscle relaxants?

A

1-3 hours

DPP
Doxacurium
Pancuronium
Pipecuronium

21
Q

Which relaxants are hydrolyzed spontaneously in the plasma?

A

Atracurium and Cisatracurium

22
Q

What types of drugs target voltage gated Na channels?

A

Local anesthetics
Antiarrhythmics
Antiepileptics

23
Q

Order of sensation loss from local anesthetics

A

In reverse order of the level of fiber myelination

Pain
Temp
Touch
Deep pressure
Motor function
24
Q

What is the mechanism that local anesthetics use to inhibit action potentials?

A

They must enter the nerve cells in the uncharged form, and the bind to Na+ channels from the intracellular side, in their ionized form.

25
Q

List the Ester linked anesthetics

How are these metabolized?

Long or short T1/2?

A 
Cocaine
Procaine
Benzocaine
Tetracaine
Cinchocaine

Esterases in plasma and tissue degrade them

Short half life

26
Q

List the Amide linked anesthetics

How are these metabolized?

Long or short T1/2?

A 
Lidocaine
Prilocaine
Bupivicaine
Articaine
QX-314

Metabolized by the liver

Long half life

27
Q

What drugs are used topically for surface anesthesia?

Where are these used?

A

Lidocaine
Tetracaine
Benzocaine
Dibucaine

Used in the nose, mouth, pharynx, bronchial tree, as a spray.
Urinary tract and uterus, for scopy procedures
Cornea

28
Q

What is infiltration anesthesia? What is it used for?

A

Local injection into tissue to anesthetize nerve branches locally. Most/any of the local anesthetics are used.

Only used for small areas and definitely not used for fingers or toes, may cause ischemic necrosis. Excessive use for large areas can cause serious systemic toxicity.

Used for minor surgery, in conjunction with a vasopressor like epinephrine.

29
Q

What drugs are used for IV regional anesthesia?

When is this technique used?

A

Lidocaine and Prilocaine

They are injected distally to a pressure cuff, remaining effective until the cuff is lifted.
Cuff must remain in place for at least 20 minutes while they are metabolized to a degree or there is risk for major toxicity.

Used for limb surgery.

30
Q

What drugs are used for Nerve Block anesthesia?

When is this technique used?

A

Most/any of the local anesthetics can be used.

the LA is injected to a nerve trunk, ie, brachial plexus, intercostal nerve, dental nerve.

Used in many surgeries,
Dental surgeries.
Pain relief.

Has a slower onset

31
Q

What anesthetics are used for spinal anesthesia?

When is the technique used?

A

Lidocaine

It is injected into the CNS of the Subarachnoid Space. Acts directly on the spinal cord as well as on the nerve roots.

May be formulated with glucose and kept cold in order to cause ‘hyperbaricity’ so that the LA sinks and does not rise higher to affect the brainstem.

Used for abdominal, pelvic, or leg surgeries.

Can be used in conjunction with general anesthesia to reduce stress, and to reduce post-op pain.

32
Q

What drugs are used for Epidural anesthesia?

When is the technique used?

A

Lidocaine or Bupivacaine

Drug is injected into the Epidural space, affecting only the spinal nerver roots.

Used abdominal, pelvic, leg surgeries,
Also administered to relieve childbirth pain.

33
Q

What are the important side effects and toxicities of Local Anesthetics?

A

Side effects occur if the drug reaches systemic circulation in too high concentrations.

Early symptoms:
Tongue/Mouth numbness
Tinnitus
Vertigo
Tremor
Confusion
CNS depression, at lower plasma LA concentrations
Confusion
LOC, coma
Resp. Depression
Cardiovascular collapse

CNS excitation, at higher conc.
Anxiety, Agitation
Vomiting
Tonic-Clonic seizures

Cardiovascular suppression,
negative: chrono, ino, dromo
peripheral vasodiulation
cardiovascular collapse

Cocaine is the exception to all of this, its overdose effects are of NE excess, and are excitatory. tachy, vasoconst. arrythmias, HTX, tremor, etc.

34
Q

What are the major components of the local anesthetics chemical structure?

A

Aromatic region

an Ester or Amide bond linking region

Ionizable Basic Amine side chain

35
Q

Interactions of local anesthetics with NMJ blockers?

A

small doses of LAs facilitate both depolarizing or non-depolarizing blockers

Large doses, cause non-specific nAChR block

36
Q

What are the MAO inhibitors

A

Tranylcypromine, Pargyline - irreversible, nonselective, cheese effect, lots of side effects. Not used.

Moclobemid: Reversible, MAO-A inhibitor, for mental depression. causes cheese effect.

Selegiline - Irreversible, MAO-B inhibitor for parkinson’s, no cheese effect, somehow discovered by people at semmelweis.

37
Q

Which local anesthetic has cardiac toxic effects if accidentally given IV?

What should be done to prevent this?

A

Bupivicaine.

Always aspirate when injecting sub-cutaneous to insure you are not in a vessel.

My pharma notes (30 decks)

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