Musculoskeletal drugs Flashcards

1
Q

Define Neuromuscular blocking drugs

A

Used to produce muscle paralysis in order to facilitate surgery or artificial ventilation ( in CNS)

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2
Q

Spasmolytic

A

A drug that reduces abnormally elevated muscle tone (spasticity) without paralysis e.g. baclofen, dantrolene, diazapem

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3
Q

major use for spasmolytic drugs

A

muscle strains (uncontrollable spasms) back pain

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4
Q

where are the GABAb receptors that Baclofen works on?

A

CNS (specifically the ventral horn of the spinal cord. specifically at the AXON TERMINAL OF THE PRESYNAPTIC AFFERENT NERVE

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5
Q

Baclofen

A

GABA agonist.

acts within the spinal cord to suppress hyperactive reflexes involved in regulation of muscle mvoement.

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6
Q

Diazepam

A

member of the benzodiazepine family. facilitating GABA mediated inhibition of motor neurons.

indicated for muscle spasm of any origin

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7
Q

Dantrolene

A

acts directly on skeletal muscle to relieve spasticity (unlike baclofen and diazepam)

blocks release of Ca form SR (decrease in SM contraction)

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8
Q

Indications for Dantrolene

A

THerapeutic uses, spasticity and malignant hyperthermia

Can relieve symptoms with MS, cerebral palsy and spinal cord injury

associated with reduction in the abillity of a skeletal muscle to contract

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9
Q

Tiazanidine

A

Alpha2 receptor agonist used for patients with brain or spinal injuries

musch less anti-hypertensive than clinidine

however causes hypetension, drosiness and drymouth

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10
Q

Spasm

A

sudden violent painful involuntary contraction of a muscle group.

involve motor neuron

(bursitis, dislocaiton, fracture, herniated disk, hypokalamia , strains)

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11
Q

Spasticity

A

Increase in passive stretch reistence of a muscle.

COnsidered permenant condition that might persis to disabling

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12
Q

causes of spasticity

A

head injurie, cerebral palsy, MS, stroke

Upper motor neuron

cerebrovascular adjacent accident
closed head injury
quadrapalegia
Spinal cord, Trauma.

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13
Q

Give a condition that baclofen is not effective in

A

relief of spasticity associated with parkinsons or in stroke

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14
Q

Give condition that Baclofen is prefered over dantrolene

A

in a patient whose spasticity is accompanied by muscle weakness

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15
Q

Explain what to do with diazepam to avoid the side effect of sedation

A

Start dose low 4mg increase to 60mg/dl

Initial therapy low dose then increase

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16
Q

Explain how dantrolene helps malignant hyperthermia

A

Malignant hyperthermia can be triggered by anesthetic and succinlycholine

Dantolene relives symptoms by blocking Ca release from SR

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17
Q

Distinguish between spasmolytic and paralytic

A

paralytic used to produce muscle paralysis to do surgery

spasmolytic used to reduce abnormally elevated muscle tone without paralysis

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18
Q

Give indications of diazempam as a spasmolytic

A

Trauma

General Muscle spasm

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19
Q

Give to therapeutic uses for dantrolene

A

spasms

malignant hyperthermia

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20
Q

Give three conditions that dantrolene can releve spasticity for

A

Cerebral palsy, MS, Spinal cord injury

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21
Q

Tetracycline mechanism of action

A

Binds reversibly to 30s subunit of bacterial ribosome and blocks the binding of a.a.-tRNA to acceptor site.

this prevents addition of a.a. to the growing peptide

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22
Q

Mechanisms of Resistence tetracycline

A

Increased efflux

Production of ribosome protection protein

enzymatic modificatio of cycline

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23
Q

Tet (AE)

A

found in gram negative bacteria

resistent to Tetra doxy mino, not tige

24
Q

Tet(K)

A

gram (+) Tetra, but not doxy mino or tige

25
Q

Tet (M)

A

gram (+) protein that renders them resistant to tetra, doxy, mino but not Tige

bulky tbutylglycylamido stops steric hindrance.

26
Q

Enzymatic inactivation

A

not important for tetracycline.

27
Q

Foods that impair Tetracycline absorption

A

Dairy antacids with multivalent cations

No effect on doxy and mino

impaired by alkaline pH because its HCl

28
Q

Places that Minocycline is very high concentration

A

Tears and salica

indicated for prophylaxis of menigococcal infections, but not 1st line

29
Q

Elimination of tetracycline

A

excreted mainly in bile and urine intestine reabsorption may contribute to maintence of serum levels

30
Q

elimination of demeclocycline

A

excreted mainly in bile and urine intestine reabsorption may contribute to maintence of serum levels

31
Q

elimination of doxycycline

A

90% in GI in inactive form

dose adjustment for renalfailure not required

32
Q

elimination of minocycline

A

Mostly metabolized in liver to inactive form

dose adjustment for renal insufficiency not required

33
Q

elmination of Tige-cycline

A

primarily excreted in bile and eliminated in feces in unchanged form

dose adjustment for renal insufficiency not required

34
Q

Tetracylcine sensitive pathogens

A

RIckettsia species
Mycoplasma pneumoniae
Chlamydophylia and chlamydia

35
Q

Special Tige-cycline indications

A

active against vancoresistant enterococci and MRSA indicated for VRE and MRSA.

36
Q

Indications for doxycycline

A

even in children less than 8 years old

chlamydial infection including STD
mycoplasma pneumonia
early lyme disease

37
Q

Tetracycline class used for S. aureus

A

Mino and tige

38
Q

Tetracycline effects on teeth and bone

A

Causes permenat gray-brown discoloration of teeth and enamel hypoplasia due to chelation and sequestion and UV-absorbing

Also impairs skeletal bone growth in the fetus and children.

contraindicated in pregnant or lactating women

39
Q

Most common side effect of tetracycline

A

Hypersensitivity to tetracycline classes

photosensitivity includes red-rashes and blistering. most common with demeclocycline.

40
Q

how should you take Tetracycline to avoid esophogeal ulceration

A

way before bedtime and with ltos of water.

41
Q

tetracycline with most hepatotoxicity

A

tetra and mino

not really doxycycline.

preggers get toxic better

42
Q

List side effects of tetracycline

A
Teeth and bone
allergic skin
GI
Liver
Renal
mortality
vertigo
43
Q

Renal adverse effects of tetracycline

A

inhibit protein synthesis and exacerbate renal failure by increasing azotemia from a.a. metabolism

Demeclocycline can cause nehrogenic diabetes insipidus (used for SIADH)

44
Q

Major side effect tigecycline

A

death

45
Q

What tetracycline is associated with reverisble vertigo

A

Minocycline

more with women

46
Q

Mechanism of action of clindamycin

A

Binds to 50S subunit interferes with transpeptidation reaction at A and P site

47
Q

Clindamycin effectiveness against certain bacteria

A

Bacteria static

anerobic infections.

Gram(-) are resistant because drug cannot permeate the bacterial outer membrane

48
Q

bioavailabillities of tetracyclines

A
Tetra 60-70
demcro 60-70
doxy 95
mino 95
tige poor
49
Q

True or false clindamycin penetrates into an abcess

A

True

50
Q

Mechanisms of resistance cliindamycin

A

mutation of ribosomal binding site
modification of ribosomal binding site by methylase (constituitively active)
Enzymatic inactivation.

51
Q

Clindamycin adverse effects

A

kills off normal flora: allowing for superinfection of C. difficile. cytotoxin can cause coltiis with lifethreatening mucosal ulcerations, fever diarrhea.

52
Q

Inidcations for clindamycin

A

treament of skin and soft tissue infections caused by streptococci and staphylococci. anaerobic infections

53
Q

Mechanism of chloramphenicol resistence

A

inactivation by acetyltransferase

54
Q

Chloramphenicol pharmokinetics

A

metabolized in liver to inactive form.

must dose compensate for liver failure

55
Q

Cloramphenicol adverse effects

A

suppression of RBC production. leads to irreversible aplastic anemia.

gray baby syndrome

56
Q

Gray baby syndrome

A

serious consequence of chloramphenicol

baby don’t glucoronidate and get vomiting flaccidity. hypothermia gray color respiratory distress and metabolic acidosis

57
Q

Chloramphenicol

A

only indicated for lifethreatening infections in people who cannot take safer alternatives because of resistence of allergies