Test 1 (Pharm) Flashcards
Pharmaco____ is how the drug affects the body (aka how the drug causes chemical and physiological effects) and Pharmaco____ is how the body affects the drug (aka ADME - Absorption/Distribution/Metabolism/Elimination)
** A pro-drug is inactive -> Active once administered
Dynamics, Kinetics
Pharmaceutical Equivalence is when a Generic name drug and Trade name drug have the SAME 1) Ingredients 2) Dosage route (Oral/IV/etc) 3) Strength (concentration)
EX: Oral Lisinopril 5mg - Zestril vs Oral Lisinopri 5mg - Generic = Same since 1, 2, and 3 are all equal
Pharmaceutical alternatives are the SAME DRUG but have either
1) A different complex (Tetracycline: hydrochloride 250mg capsule vs Tetracycline: Phosphate 250mg capsule)
2) A different dosage form (Quinidine sulfate 200mg tablet vs Quinidine sulfate 200mg capsule)
3) A different strength (Vancomycin 250mg capsule vs Vancomycin 125mg/5ml Liquid)
Along with Pharmaceutical Equivalence, Therapeutic Equivalence has all of the 3 Pharmaceutical criteria PLUS the same 1) Clinical effect 2) Safety profile
Finally, there is Bio Equivalence that is involved with the same RATE and ABSORPTION patterns
^** If ALL 3 Equivalences are met, then the Trade name drug and Generic name drug are the EXACT SAME
FDA rated drugs with an ___ rating mean generic and trade name drugs are the same
Know this concept
A
Scheduled/Controlled drugs (which are found in the Legend category) are C-1 to C-5 with C-___ being the most likely drug to be abused/addiction
C-1 (C1 is the highest risk and C5 is the lowest risk out of the Controlled substances)
Non controlled legend medications expire at either ___ months or number of refills reached
^** Is partial filling allowed? Is there a legal limit on number of refills or quantity dispensed during its 12 month life-span?
Controlled legend medications expire at either ___ months of number of refills reached
^** Is there a legal limit on number of refills? Is there a legal limit on how often you can get a refill aka quantity?
C-3 to C-5 can have ___ refills and C-2 can have ___ refills
C3-C5 must have a patient wait ____ days before they can get their next refill and C-2 drugs must have the patient wait ____ days before they can get their next refill
** Partial filling is possible for C3-C5 but not C2
** Also know docs can call in for prescriptions for all legend drugs EXCEPT for C2 (unless it is an emergency)
12
Yes, No
6
Yes, Yes
5, 0
90, 30
KNOW ABBREVIATIONS AND WEIGHT CONVERSIONS
Gm Mg (1/1000 gm) Mcg (1/1000 mg) MEq Lb Kg -> 1kg = \_\_\_ lbs
Tsp -> \_\_\_ ml Tbsp -> \_\_\_ tsp Ounce (OZ) -> \_\_\_ tsp Quart = 2 pints Pint = \_\_\_ Oz Liter = \_\_\_ ml Gallon (G) = \_\_\_ quarts or 8 pints
2.2
5ml 3tsp (aka 15ml) 6tsp (aka 30 ml) 16 1000 4
MORE ABBREVIATIONS
Qd Bid Tid Qid Qod Q"x"h M/T/W/Th(R)/F/Sa/S
Qam Qpm Qhs Prn Ac Pc
Od Os Ou Ad As Au Gtt
Po Sl ** iv Im Sq Pr NGT OGT Ut dict (Ud) Tra Kvo
KNOW THESE
Sl = sublingually aka under the tongue
Normal Saline (NS) contains 0.90% NaCl so half of NS is 0.45% etc…
D”X”W such as D5W has the X tell you the percentage of dextrose in solution so for D5W there is 5% dextrose in solution aka 5 grams of dextrose in every 100 ml of fluid
More concepts
The defining feature of ____ are the presence of the DNA-binding domains that allow them to bind to specific DNA sequences at ___ or ____ regions of the DNA that are adjacent to the coding sequences of the regulated gene; allowing them control the rate of transcription via promoting or inhibiting ____ activity
The specific DNA sequence that they bind to is called a ___
Transcription factors, enhancer or promoter, RNA polymerase
Response element (usually TATA)
Trimeric G proteins have GTPase activity (the ability to hydrolyze GTP) and ____s allow GTP to be exchanged for GDP and therefore the alpha subunit becomes active
___s allow GDP be be exchanged for GTP (aka GTP -> GDP) causing inactivation
^** So GTP hydrolysis by the Alpha subunit causes _____ activity of the GPCR
Gs family activates ___ and ___ Src tyrosine kinase
Gi family inhibits ___ and ___ Src tyrosine kinase
Gq family activates ____
GEFs
GAPs
Decreased
AC, activates
AC, activates
PLC
Inactive PKA has ___ subunits and active PKA has ___ subunits
Inactive = 2 Regulatory and 2 Catalytic
Active = 2 Catalytic
Protein Kinases phosphorylate aka activate and ____s dephosphorylate
During GPCR desensitization, a ligand (agonist) binds to the GPCR and activates the Gs subunit
After the G protein is released to cause signaling transduction, ___ regulates the GPCRs activity by binding and phosphorylating agonist-activated receptors causing ___ to bind to the receptor
The BetaArr-Receptor complex binds to coated pits (which turn into endosomes) causing internalization and dissociation of the agonistic ligand causing no more affinity for B-Arr and since it does not bind anymore, dephosphorylation occurs and the receptor moves back to the membrane to become activated once again
The problem occurs when prolonged exposure to an agonist happens which causes the internalized GPCRs in their endosomes to have enough time to merge with lysosomes causing the entire receptor to be destroyed and therefore downregulation
Phosphatase (P’ase)
GRK (G protein-coupled receptor kinase)
B-arrestin
___ ligands include Ach, NE, E, Dopa, Ser, Hist, ACTH, Bradykinin, Angiotensin, Opioids, GABA, Glutamate, Leukotrienes, TxA2, ADP, ATP, Adenosine
___ ligands include IGF-1, VEGF, EGF, NGF, PDGF, and INSULIN
^** Insulin and IGF have 2 chains (alpha and beta) and most other RTKs have 1
____ ligands include Growth hormone (somatotropin), Erythropoietin, Leptin, Interferons AKA cytokines*
____ ligands include Steroid hormones, Thyroid hormones, Vitamin D, Vitamin A, and Lipid mediators (such as free fatty acids and their products)
GPCR
RTK
JAK-STAT
Nuclear
Like trimeric GTPases involved with GPCRs, ____ is a monomeric GTPase involved with RTKs that helps phosphorylate protein targets in the nucleus, plasma membrane, and cytoplasm that causes alterations in gene transcription and protein activity
The adaptor protein (which brings signaling molecules together) called ____ contains an SH__ domain that binds to the phosphorylated RTK and an SH___ domain that binds to the proline-rich sequences
Just like in GPCRs, ___ activate the monomeric GTPase (Ras) by causing GDP to be replaced by GTP and ___ inactivate monomeric GTPases (Ras) by hydrolysis of GTP
^** The common GEF in this mechanism is called ___
Ras
Grb2 (Growth factor receptor-bound protein 2), SH2, SH3
GEFs, GAPs
Sos
So if you were to have a mutation that affects the GTPase activity of Ras (aka a decrease in GAP), you could get excessive stimulation leading to cancer and most commonly _____ are seen
^** Because remember, GTPase means hydrolysis of GTP -> GDP and therefore if you can no longer convert GTP to the inactive GDP, then excessive stimulation will occur
***GRB2 -> Sos (GEF) -> Active Ras -> Raf -> MEK -> ERK -> Changes in transcription
A point mutation in Raf often leads to ____
One way to treat a patient with a mutation causing excessive cell growth is to either inhibit the growth factor’s receptor or the growth factor ligand itself via ____ OR you could inhibit the kinase activity such as inhibiting RAF1 via _____ inhibitors
Pancreatic adenocarcinomas
Melanomas
Monoclonal Abs, Multikinase
Growth hormones and ____ molecules bind to RTKs that cause JAK to become activated causing the phosphorylation of tyrosine residues on the RTKs
Next, STAT is recruited and the JAK helps phosphorylate STAT as well and then it travels to the nucleus to regulate transcription
**JAK inhibitors can aid in allergic and autoimmune disorders
Cytokine
Steroid/Nuclear receptors have a ____ (delayed or immediate?) action on gene transcription
Nuclear receptors become activated (stabilized and converted to active configuration) when a steroid binds to the ligand-binding domain causing ___ to be dissociated
Now the receptor can translocate into the nucleus with an active DNA-binding domain that binds to the specific gene sequence and a active transcription activating domain that recruits RNA pol which are both needed for altered gene trasncription
Delayed
Hsp90 (heat shock protein)
___-gated channels are regulated by membrane potential changes and ____-gated channels are regulated by ligands binding
Voltage gated Na+ channels and voltage gated Ca2+ channels exist and ___ channels are the ones that deal with cardiac and smooth muscle cells
Name if the NT is excitatory or inhibitory for Ligand-gated channels
1) Ach
2) GABA
3) Glycine
4) Glutamate
^** Excitatory NTs open ___ channels and inhibitory NTs open ___ channels
Voltage, Ligand
Ca2+
1) Excitatory
2) Inhibitory
3) Inhibitory
4) Excitatory
Cation, Anion
Nicotinic Ach receptors allow ____ influx to ___polarize the membrane and are located at ___ muscles and ____ cells
GABA-A receptors allow ____ influx to ___polarize the membrane causing synaptic inhibition in the CNS
Na+, DEpolarize, Skeletal, Neuronal
Cl- HYPERpolarize