Use of granisetron transdermal system in the prevention of chemotherapy-induced nausea and vomiting: a review

Figures & data

Table 1 Emesis risk level of antineoplastic drugs

Level 1 (<10%)	Level 2 (10%–30%)	Level 3 (31%–90%)	Level 4 (>90%)
Bleomicin	Bortezimib	Carboplatin	Carmustine
Busulfan	Cetuximab	Cyclophoshamide	Cisplatin
Vinbalstine	Cytarabine	(<1.5 g/m^2)	Cyclophosphamide
Vinorelbine	(<100 mg/m^2)	Cytarabine	(>1.5 g/m^2)
Fludrabine	Docetaxel	Daunorubicin	Dacarbazine
Cladribine	Etoposide	Doxorubicin	Mechlorethamine
Bevacizumab	Flouracil	Epirubicin	Streptozocin
	Gemcitabine	Idarubicin
	Ixabepilone	Ifosfamide
	Lapatinib	Irinotecan
	Methotrexate	Oxaliplatin
	Mitomicyn
	Mitoxantrone
	Paclitaxel
	Pemetrexed
	Temsirolimus
	Topotecan
	Tastuzumab

Table 2 Pharmacokinetics parameters of oral and transdermal granisetron^49,50,61

Mean	Granisetron 2 mg oral daily		Granisetron patch 52 cm^2
	Day 1	Day 5
Cmax ng/mL	5.2	5.5	4.0–2.2
tmax (hours)	1.5	2.0	48
Cavg (ng/mL)	2.14	2.6	2.23
AUC (0→∞) ng·h/mL	65	98	420
t½ (hours)	6.4	7.9	35.9

Abbreviations: C_max, maximal mean concentration; t_max, peak of maximal concentration; C_avg, average concentration; AUC, area under the curve concentration; t_½, half-life.

Figure 1 Plasma concentration of granisetron after application of the transdermal patch of 52 cm² for 6 days of treatment. Based on study 392MD/11/C.⁴⁹

Table 3 Rate of acute emesis control and related-treatment side adverse effects in controlled clinical trials^56,59,60

		Transdermal granisetron	Oral granisetron
Phase II (N = 210)	Complete controla	48.3%	59.5%
	Related-treatment SAE	4.5%	9.4%
	Constipation	nr	nr
	Headache	3.4%	4.7%
Phase III (N = 641)	Complete control	60.2%	64.8%
	Related-treatment SAE	7.9%	5.6%
	Constipation	6.6%	3.1%
	Headache	0.3%	2.5%

Note: No statistically significant differences in all items in both trials.

a Complete control: no more than mild nausea, no vomiting, no rescue medication.

Abbreviations: nr, not reported in available documentation; SAE, side adverse effects.

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